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Chemical Structure| 668270-12-0 Chemical Structure| 668270-12-0

Structure of Linagliptin
CAS No.: 668270-12-0

Chemical Structure| 668270-12-0

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Linagliptin, a purine and quinazoline derivative, can inhibit DPP-4 with IC50 of 1 nM. It functions as an incretin and is used as a hypoglycemic agents in the treatment of type 2 diabetes mellitus.

Synonyms: BI 1356; GSK2118436

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Product Details of Linagliptin

CAS No. :668270-12-0
Formula : C25H28N8O2
M.W : 472.54
SMILES Code : CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
Synonyms :
BI 1356; GSK2118436
MDL No. :MFCD14635356
InChI Key :LTXREWYXXSTFRX-QGZVFWFLSA-N
Pubchem ID :10096344

Safety of Linagliptin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P280-P305+P351+P338-P310

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human cardiomyocytes 100 mM 30 minutes To evaluate the effect of Linagliptin on cardiomyocyte passive stiffness, results showed that Linagliptin significantly reduced cardiomyocyte passive stiffness. PMC7812306
human cardiomyocytes 100 mM 2 hours To evaluate the effect of Linagliptin on DPP-4-mediated titin cleavage, results showed that Linagliptin completely prevented DPP-4-induced titin cleavage. PMC7812306

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Swiss mice Morphine dependence model Intraperitoneal injection 10 and 20 mg/kg Once daily for 8 consecutive days Linagliptin significantly reduced morphine withdrawal symptoms (jumping behavior) in mice and alleviated depressive and anxiety behaviors during short-term and long-term morphine withdrawal. PMC9028142
ZSF1 rats MetS-induced cardiac disease model Oral 83 mg/kg once daily for 4 weeks To evaluate the effect of Linagliptin on left ventricular stiffness, results showed that Linagliptin significantly improved left ventricular relaxation, reduced cardiomyocyte passive stiffness, and decreased cardiac fibrosis. PMC7812306
db/db mice type 2 diabetes model Oral 10 mg/kg Once daily for 8 weeks To assess the effect of Linagliptin on glomerular autophagy in a model of type 2 diabetes, the results showed that Linagliptin alone or in combination with Empagliflozin enhanced glomerular autophagy, mitigated glomerular sclerosis and podocyte injury, and slowed the growth of albuminuria. PMC7215949
C57BL6/ApoE-/- mice High fat diet-induced metabolic disease model Oral gavage 10 mg/kg Once daily for 28 days To validate the regulatory effect of DPP4 inhibitor on insulin-induced vascular oxidative stress in vivo, results showed DPP4i pretreatment reversed the effects of insulin on vascular oxidative stress PMC7212010

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02183376 Hepatic Insufficiency PHASE1 COMPLETED - -
NCT01778049 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT02183532 Healthy Phase 1 Completed - -
NCT01778049 - Completed - -
NCT00819091 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01703286 Diabetes Mellitus, Type 2 Phase 1 Completed - Germany ... More >> 1218.105.001 Boehringer Ingelheim Investigational Site Neuss, Germany Less <<
NCT00819091 - Completed - -
NCT02173639 Healthy Phase 1 Completed - -
NCT01703286 - Completed - -
NCT01087502 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT02173652 Healthy Phase 1 Completed - -
NCT01087502 - Completed - -
NCT01734785 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01708902 - Completed - -
NCT02821910 Healthy Phase 1 Completed - Germany ... More >> Boehringer Ingelheim Investigational Site Biberach, Germany Less <<
NCT02183428 Healthy Phase 1 Completed - -
NCT01708902 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01215097 Diabetes Mellitus, Type 2 Phase 3 Completed - China ... More >> 1218.65.86007 Boehringer Ingelheim Investigational Site Beijing, China 1218.65.86011 Boehringer Ingelheim Investigational Site Chongqing, China 1218.65.86008 Boehringer Ingelheim Investigational Site Dalian, China 1218.65.86010 Boehringer Ingelheim Investigational Site Fuzhou, China 1218.65.86014 Boehringer Ingelheim Investigational Site Hangzhou, China 1218.65.86005 Boehringer Ingelheim Investigational Site Hefei, China 1218.65.86006 Boehringer Ingelheim Investigational Site Hefei, China 1218.65.86012 Boehringer Ingelheim Investigational Site Nanjing, China 1218.65.86001 Boehringer Ingelheim Investigational Site Shanghai, China 1218.65.86002 Boehringer Ingelheim Investigational Site Shanghai, China 1218.65.86003 Boehringer Ingelheim Investigational Site Shanghai, China 1218.65.86004 Boehringer Ingelheim Investigational Site Suzhou, China 1218.65.86015 Boehringer Ingelheim Investigational Site Wenzhou, China 1218.65.86009 Boehringer Ingelheim Investigational Site Wuhan, China 1218.65.86013 Boehringer Ingelheim Investigational Site Yangzhou, China Malaysia 1218.65.60002 Boehringer Ingelheim Investigational Site Johor Bahru,, Malaysia 1218.65.60001 Boehringer Ingelheim Investigational Site Kelantan, Malaysia Philippines 1218.65.63001 Boehringer Ingelheim Investigational Site Marikina, Philippines 1218.65.63002 Boehringer Ingelheim Investigational Site San Juan, Philippines Less <<
NCT01215097 - Completed - -
NCT01734785 - Completed - -
NCT00800683 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT00621140 - Completed - -
NCT02183493 Healthy PHASE1 COMPLETED - -
NCT02191228 Renal Insufficiency Phase 1 Completed - -
NCT00800683 - Completed - -
NCT02221414 Healthy Phase 1 Completed - -
NCT02183441 Healthy Phase 1 Completed - -
NCT00621140 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT02489968 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT03433248 Type2 Diabetes Phase 4 Recruiting December 1, 2020 Netherlands ... More >> VU University Medical Center Recruiting Amsterdam, Noord-Holland, Netherlands, 1081HV Contact: Michaël JB van Baar, MD    +31 20 444 4709    m.vanbaar@vumc.nl    Contact: Daniël H van Raalte, MD PhD    +31 20 444 0534    d.vanraalte@vumc.nl    Principal Investigator: Mark HH Kramer, MD PhD          Principal Investigator: Daniël H van Raalte, MD PhD Less <<
NCT02221401 Healthy Phase 1 Completed - -
NCT02489968 - Completed - -
NCT01438814 Diabetes Mellitus, Type 2 Phase 4 Completed - -
NCT01947153 - Completed - -
NCT02220647 Healthy Phase 1 Completed - -
NCT01897532 Diabetes Mellitus, Type 2 Phase 4 Completed - -
NCT01438814 - Completed - -
NCT02897349 Diabetes Mellitus, Type 2 Phase 3 Active, not recruiting January 30, 2019 China ... More >> China-Japan Friendship Hospital Beijing, China, 100029 Beijing Tongren Hospital Beijing, China, 100730 The General Hospital of Chinese People's Armed Police Forces Beijing, China, 100854 First Hospital of Jilin University Changchun, China, 130021 Fuzhou General Hospital of Nanjing Militray Command Fuzhou, China, 350025 Third Affiliated Hospital of Guangzhou Medical University Guangzhou, China, 510150 The Affiliated Hospital of Guizhou Medical University Guiyang, China, 550004 Hangzhou Second People's Hospital Hangzhou, China, 310015 General Hospital of Jinan Military Area Jinan, China, 250000 Nanjing First Hospital Nanjing, China, 210006 The affiliated hospital of medicalcollege qingdao university Qingdao, China, 266005 Centre Hospital of Putuo District, Shanghai Shanghai, China, 200062 Shanghai Tenth People's Hospital Shanghai, China, 200072 Yangpu Hospital, Tongji University Shanghai, China, 200090 Second Hospital Affiliated to Shantou Medical University Shantou, China, 515041 Shengjing Hospital of China Medical University Shengyang, China, 110072 Siping Central People's Hospital Siping, China, 136000 The First Affiliated Hospital of Soochow University Suzhou, China, 215006 Nankai University Affiliated Hospital Tianjin, China, 300000 The 2nd Hospital of Tianjin Medical University Tianjin, China, 300000 Tianjin Medical University General Hospital Tianjin, China, 30052 Renmin Hospital of Wuhan University Wuhan, China, 430060 First Affiliated Hospital of Xiamen University Xiamen, China, 361003 the first people hospital of Yue Yang Yueyang, China, 414000 Affiliated Hospital of Jiangsu University Zhenjiang, China, 212013 Less <<
NCT01947153 Healthy Phase 1 Completed - Russian Federation ... More >> 1288.21.1 Boehringer Ingelheim Investigational Site St. Petersburg, Russian Federation Less <<
NCT02172222 Healthy Phase 1 Completed - -
NCT01194830 - Completed - -
NCT01194830 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01903356 - Completed - Korea, Republic of ... More >> One or multiple Investigational sites, Korea, Republic of Less <<
NCT00602472 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT02183636 Healthy Phase 1 Completed - -
NCT01342484 - Completed - -
NCT00602472 - Completed - -
NCT01969084 Type II Diabetes Mellitus Phase 4 Completed - United States, Massachusetts ... More >> Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 Less <<
NCT01969084 - Completed - -
NCT01512979 Diabetes Mellitus, Type 2 Phase 4 Completed - -
NCT01888796 Diabetes Mellitus Type 2 (T2DM... More >>) Left Ventricular Diastolic Dysfunction Less << Phase 3 Terminated(bad recruitment of ... More >>suitable participants, just 8 patients in one year) Less << - Germany ... More >> Department of Internal Medicine I, University Hospital Aachen, Germany, 52074 Less <<
NCT01342484 Diabetes Mellitus, Type 2 Phase 2 Completed - United States, Texas ... More >> 1218.56.01006 Boehringer Ingelheim Investigational Site San Antonio, Texas, United States United States, Virginia 1218.56.01004 Boehringer Ingelheim Investigational Site Norfolk, Virginia, United States Canada, Quebec 1218.56.11001 Boehringer Ingelheim Investigational Site Montreal, Quebec, Canada France 1218.56.33003 Boehringer Ingelheim Investigational Site Fort de France cedex, France 1218.56.33006 Boehringer Ingelheim Investigational Site Rouen, France Guatemala 1218.56.50202 Boehringer Ingelheim Investigational Site Guatemala, Guatemala 1218.56.50203 Boehringer Ingelheim Investigational Site Guatemala, Guatemala Italy 1218.56.39005 Boehringer Ingelheim Investigational Site Firenze, Italy Korea, Republic of 1218.56.82005 Boehringer Ingelheim Investigational Site Busan, Korea, Republic of 1218.56.82001 Boehringer Ingelheim Investigational Site Seoul, Korea, Republic of 1218.56.82002 Boehringer Ingelheim Investigational Site Seoul, Korea, Republic of 1218.56.82003 Boehringer Ingelheim Investigational Site Suwon, Korea, Republic of Mexico 1218.56.52008 Boehringer Ingelheim Investigational Site Chihuahua, Mexico 1218.56.52002 Boehringer Ingelheim Investigational Site Guadalajara, Mexico 1218.56.52001 Boehringer Ingelheim Investigational Site León, Mexico 1218.56.52003 Boehringer Ingelheim Investigational Site Monterrey, Mexico 1218.56.52004 Boehringer Ingelheim Investigational Site Oaxaca, Mexico Poland 1218.56.48002 Boehringer Ingelheim Investigational Site Gdansk, Poland 1218.56.48001 Boehringer Ingelheim Investigational Site Gliwice, Poland 1218.56.48004 Boehringer Ingelheim Investigational Site Warszawa, Poland 1218.56.48003 Boehringer Ingelheim Investigational Site Wroclaw, Poland Russian Federation 1218.56.70001 Boehringer Ingelheim Investigational Site Moscow, Russian Federation 1218.56.70003 Boehringer Ingelheim Investigational Site Saratov, Russian Federation 1218.56.70004 Boehringer Ingelheim Investigational Site Ufa, Russian Federation 1218.56.70006 Boehringer Ingelheim Investigational Site Yekaterinburg, Russian Federation Less <<
NCT01512979 - Completed - -
NCT01581931 Healthy Phase 1 Completed - Germany ... More >> 1288.20.1 Boehringer Ingelheim Investigational Site Biberach, Germany Less <<
NCT03259490 Healthy Phase 1 Completed - Germany ... More >> Humanpharmakologisches Zentrum Biberach Biberach, Germany, 88397 Less <<
NCT01581931 - Completed - -
NCT01012037 Diabetes Mellitus, Type 2 Phase 2 Completed - -
NCT01243424 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01012037 - Completed - -
NCT01276327 - Completed - -
NCT01792518 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01792518 - Completed - -
NCT00915772 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT00601250 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT00601250 - Completed - -
NCT03642184 New Onset Diabetes After Trans... More >>plant Kidney Transplant; Complications Less << Phase 4 Recruiting December 31, 2020 China, Shanghai ... More >> Department of nephrology, endocrinology and kidney transplantation , Ren Ji Hospital, Shanghai Jiao Tong University School of Medicine Recruiting Shanghai, Shanghai, China, 200127 Contact: Shan Mou, Dr.    +8613918221242    shan_mou@126.com Less <<
NCT03629054 Healthy Phase 1 Completed - Germany ... More >> Humanpharmakologisches Zentrum Biberach Biberach, Germany, 88397 Less <<
NCT00915772 - Completed - -
NCT01383356 Diabetes Mellitus, Type 2 Phase 1 Completed - Canada, Ontario ... More >> 1288.19.1 Boehringer Ingelheim Investigational Site Toronto, Ontario, Canada Less <<
NCT01383356 - Completed - -
NCT01276327 Healthy Phase 1 Completed - Germany ... More >> 1264.14.1 Boehringer Ingelheim Investigational Site Biberach, Germany Less <<
NCT01547104 Diabetes Mellitus Type 2 Phase 4 Unknown October 2012 Germany ... More >> ikfe GmbH Recruiting Mainz, Rhineland-Palatinate, Germany, 55116 Contact: Thomas Forst, MD, PhD    + 49 6131 57636 ext 16    ThomasF@ikfe.de    Contact: Daniela Sachsenheimer, MD    + 49 6131 57636 ext 46    DanielaS@ikfe.de    Sub-Investigator: Daniela Sachsenheimer, MD          Sub-Investigator: Stephanie Helleberg, MD          Sub-Investigator: Stefan Diessel          Sub-Investigator: Michael Mitry, MD Less <<
NCT00954447 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01845077 Healthy Phase 1 Completed - United States, Texas ... More >> 1288.8.1 Boehringer Ingelheim Investigational Site Austin, Texas, United States Less <<
NCT01707147 - Completed - Korea, Republic of ... More >> Multiple Locations, Korea, Republic of Less <<
NCT01189201 Healthy Phase 1 Completed - Germany ... More >> 1275.3.1 Boehringer Ingelheim Investigational Site Biberach, Germany Less <<
NCT01189201 - Completed - -
NCT00996658 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT00996658 - Completed - -
NCT02453555 Diabetes Mellitus, Type 2 Phase 3 Completed - Japan ... More >> 1275.19.81519 Boehringer Ingelheim Investigational Site Aichi, Nagoya, Japan 1275.19.81536 Boehringer Ingelheim Investigational Site Chiba, Kashiwa, Japan 1275.19.81530 Boehringer Ingelheim Investigational Site Fukuoka, Fukuoka, Japan 1275.19.81529 Boehringer Ingelheim Investigational Site Fukuoka, Itoshima, Japan 1275.19.81531 Boehringer Ingelheim Investigational Site Fukuoka, Kurume, Japan 1275.19.81504 Boehringer Ingelheim Investigational Site Fukushima, Koriyama, Japan 1275.19.81528 Boehringer Ingelheim Investigational Site Hiroshima, Hiroshima, Japan 1275.19.81501 Boehringer Ingelheim Investigational Site Hokkaido, Sapporo, Japan 1275.19.81502 Boehringer Ingelheim Investigational Site Hokkaido, Sapporo, Japan 1275.19.81503 Boehringer Ingelheim Investigational Site Hokkaido, Sapporo, Japan 1275.19.81532 Boehringer Ingelheim Investigational Site Hokkaido, Sapporo, Japan 1275.19.81505 Boehringer Ingelheim Investigational Site Ibaraki, Koga, Japan 1275.19.81533 Boehringer Ingelheim Investigational Site Ibaraki, Naka, Japan 1275.19.81516 Boehringer Ingelheim Investigational Site Kanagawa, Kawasaki, Japan 1275.19.81537 Boehringer Ingelheim Investigational Site Kanagawa, Sagamihara, Japan 1275.19.81538 Boehringer Ingelheim Investigational Site Kanagawa, Yokohama, Japan 1275.19.81520 Boehringer Ingelheim Investigational Site Kyoto, Kyoto, Japan 1275.19.81521 Boehringer Ingelheim Investigational Site Kyoto, Kyoto, Japan 1275.19.81539 Boehringer Ingelheim Investigational Site Kyoto, Kyoto, Japan 1275.19.81517 Boehringer Ingelheim Investigational Site Nagano, Matsumoto, Japan 1275.19.81518 Boehringer Ingelheim Investigational Site Nagano, Matsumoto, Japan 1275.19.81525 Boehringer Ingelheim Investigational Site Osaka, Higashi-Osaka, Japan 1275.19.81523 Boehringer Ingelheim Investigational Site Osaka, Osaka, Japan 1275.19.81526 Boehringer Ingelheim Investigational Site Osaka, Osaka, Japan 1275.19.81527 Boehringer Ingelheim Investigational Site Osaka, Osaka, Japan 1275.19.81540 Boehringer Ingelheim Investigational Site Osaka, Osaka, Japan 1275.19.81522 Boehringer Ingelheim Investigational Site Osaka, Suita, Japan 1275.19.81524 Boehringer Ingelheim Investigational Site Osaka, Takatsuki, Japan 1275.19.81535 Boehringer Ingelheim Investigational Site Saitama, Hanno, Japan 1275.19.81506 Boehringer Ingelheim Investigational Site Saitama, Kawagoe, Japan 1275.19.81507 Boehringer Ingelheim Investigational Site Saitama, Saitama, Japan 1275.19.81534 Boehringer Ingelheim Investigational Site Saitama, Tokorozawa, Japan 1275.19.81509 Boehringer Ingelheim Investigational Site Tokyo, Chiyoda-ku, Japan 1275.19.81508 Boehringer Ingelheim Investigational Site Tokyo, Chuo-ku, Japan 1275.19.81512 Boehringer Ingelheim Investigational Site Tokyo, Chuo-ku, Japan 1275.19.81515 Boehringer Ingelheim Investigational Site Tokyo, Hachioji, Japan 1275.19.81511 Boehringer Ingelheim Investigational Site Tokyo, Koto-ku, Japan 1275.19.81513 Boehringer Ingelheim Investigational Site Tokyo, Meguro-ku, Japan 1275.19.81514 Boehringer Ingelheim Investigational Site Tokyo, Shinagawa-ku, Japan 1275.19.81510 Boehringer Ingelheim Investigational Site Tokyo, Shinjuku-ku, Japan Less <<
NCT00954447 - Completed - -
NCT01826370 Diabetes Mellitus, Type 2 TERMINATED 2025-10-13 Boehringer Ingelheim Investiga... More >>tional Site 43, Agoo, La Union, Philippines|Boehringer Ingelheim Investigational Site 40, Angeles City, Pampanga, Philippines|Boehringer Ingelheim Investigational Site 31, Angono, Rizal, Philippines|Boehringer Ingelheim Investigational Site 32, Antipolo, Rizal, Philippines|Boehringer Ingelheim Investigational Site 27, Aparri, Cagayan, Philippines|Boehringer Ingelheim Investigational Site 4, Batangas, Philippines|Boehringer Ingelheim Investigational Site 48, Butuan City, Agusan del Norte, Philippines|Boehringer Ingelheim Investigational Site 12, Cabanatuan, Nueva Ecija, Philippines|Boehringer Ingelheim Investigational Site 23, Cagayan de Oro, Philippines|Boehringer Ingelheim Investigational Site 3, Caloocan, Philippines|Boehringer Ingelheim Investigational Site 42, Cardona, Rizal, Philippines|Boehringer Ingelheim Investigational Site 25, Cebu, Philippines|Boehringer Ingelheim Investigational Site 44, Dagupan, Pangasinan, Philippines|Boehringer Ingelheim Investigational Site 49, Iligan City, Lanao del Norte, Philippines|Boehringer Ingelheim Investigational Site 2, Iloilo, Philippines|Boehringer Ingelheim Investigational Site 45, Iriga City, Camarines Sur, Philippines|Boehringer Ingelheim Investigational Site 20, Laoag, Ilocos Norte, Philippines|Boehringer Ingelheim Investigational Site 24, Las Pinas, Philippines|Boehringer Ingelheim Investigational Site 7, Legazpi, Albay, Philippines|Boehringer Ingelheim Investigational Site 35, Lucena, Quezon, Philippines|Boehringer Ingelheim Investigational Site 1, Makati, Philippines|Boehringer Ingelheim Investigational Site 39, Malolos, Bulacan, Philippines|Boehringer Ingelheim Investigational Site 37, Mandaluyong City, Philippines|Boehringer Ingelheim Investigational Site 28, Manila, Philippines|Boehringer Ingelheim Investigational Site 5, Marikina, Philippines|Boehringer Ingelheim Investigational Site 16, Meycauyan, Bulacan, Philippines|Boehringer Ingelheim Investigational Site 47, Naga City, Camarines Sur, Philippines|Boehringer Ingelheim Investigational Site 15, Olongapo, Philippines|Boehringer Ingelheim Investigational Site 10, Pampanga, Philippines|Boehringer Ingelheim Investigational Site 19, Paranaque, Philippines|Boehringer Ingelheim Investigational Site 51, Pasay City, Philippines|Boehringer Ingelheim Investigational Site 30, Pasig, Philippines|Boehringer Ingelheim Investigational Site 34, Puerto Princesa, Palawan, Philippines|Boehringer Ingelheim Investigational Site 26, Quezon City, Philippines|Boehringer Ingelheim Investigational Site 11, Rosales, Pangasinan, Philippines|Boehringer Ingelheim Investigational Site 21, San Fernando, La Union, Philippines|Boehringer Ingelheim Investigational Site 9, San Fernando, Pampanga, Philippines|Boehringer Ingelheim Investigational Site 13, San Jose, Nueva Ecija, Philippines|Boehringer Ingelheim Investigational Site 29, San Juan, Philippines|Boehringer Ingelheim Investigational Site 8, San Pablo, Laguna, Philippines|Boehringer Ingelheim Investigational Site 50, San Pedro, Laguna, Philippines|Boehringer Ingelheim Investigational Site 41, Santiago city, Isabela, Philippines|Boehringer Ingelheim Investigational Site 36, Sogod, Southern Leyte, Philippines|Boehringer Ingelheim Investigational Site 38, Sta.Maria, Bulacan, Philippines|Boehringer Ingelheim Investigational Site 6, Tacloban, Philippines|Boehringer Ingelheim Investigational Site 33, Tagbilaran, Bohol, Philippines|Boehringer Ingelheim Investigational Site 14, Tuguegarao, Cagayan, Philippines|Boehringer Ingelheim Investigational Site 18, Urdaneta, Pangasinan, Philippines|Boehringer Ingelheim Investigational Site 46, Valencia City Bukidnon, Philippines|Boehringer Ingelheim Investigational Site 17, Valenzuela, Bulacan, Philippines|Boehringer Ingelheim Investigational Site 22, Zamboanga, Philippines Less <<
NCT02183480 Healthy Phase 1 Completed - -
NCT02223026 Healthy Phase 1 Completed - -
NCT01845077 - Completed - -
NCT01084005 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01216397 Healthy Phase 1 Completed - Germany ... More >> 1288.6.1 Boehringer Ingelheim Investigational Site Ingelheim, Germany Less <<
NCT01084005 - Completed - -
NCT02183584 Healthy Phase 1 Completed - -
NCT01216397 - Completed - -
NCT01826370 Diabetes Mellitus, Type 2 TERMINATED 2025-10-13 Boehringer Ingelheim Investiga... More >>tional Site 43, Agoo, La Union, Philippines|Boehringer Ingelheim Investigational Site 40, Angeles City, Pampanga, Philippines|Boehringer Ingelheim Investigational Site 31, Angono, Rizal, Philippines|Boehringer Ingelheim Investigational Site 32, Antipolo, Rizal, Philippines|Boehringer Ingelheim Investigational Site 27, Aparri, Cagayan, Philippines|Boehringer Ingelheim Investigational Site 4, Batangas, Philippines|Boehringer Ingelheim Investigational Site 48, Butuan City, Agusan del Norte, Philippines|Boehringer Ingelheim Investigational Site 12, Cabanatuan, Nueva Ecija, Philippines|Boehringer Ingelheim Investigational Site 23, Cagayan de Oro, Philippines|Boehringer Ingelheim Investigational Site 3, Caloocan, Philippines|Boehringer Ingelheim Investigational Site 42, Cardona, Rizal, Philippines|Boehringer Ingelheim Investigational Site 25, Cebu, Philippines|Boehringer Ingelheim Investigational Site 44, Dagupan, Pangasinan, Philippines|Boehringer Ingelheim Investigational Site 49, Iligan City, Lanao del Norte, Philippines|Boehringer Ingelheim Investigational Site 2, Iloilo, Philippines|Boehringer Ingelheim Investigational Site 45, Iriga City, Camarines Sur, Philippines|Boehringer Ingelheim Investigational Site 20, Laoag, Ilocos Norte, Philippines|Boehringer Ingelheim Investigational Site 24, Las Pinas, Philippines|Boehringer Ingelheim Investigational Site 7, Legazpi, Albay, Philippines|Boehringer Ingelheim Investigational Site 35, Lucena, Quezon, Philippines|Boehringer Ingelheim Investigational Site 1, Makati, Philippines|Boehringer Ingelheim Investigational Site 39, Malolos, Bulacan, Philippines|Boehringer Ingelheim Investigational Site 37, Mandaluyong City, Philippines|Boehringer Ingelheim Investigational Site 28, Manila, Philippines|Boehringer Ingelheim Investigational Site 5, Marikina, Philippines|Boehringer Ingelheim Investigational Site 16, Meycauyan, Bulacan, Philippines|Boehringer Ingelheim Investigational Site 47, Naga City, Camarines Sur, Philippines|Boehringer Ingelheim Investigational Site 15, Olongapo, Philippines|Boehringer Ingelheim Investigational Site 10, Pampanga, Philippines|Boehringer Ingelheim Investigational Site 19, Paranaque, Philippines|Boehringer Ingelheim Investigational Site 51, Pasay City, Philippines|Boehringer Ingelheim Investigational Site 30, Pasig, Philippines|Boehringer Ingelheim Investigational Site 34, Puerto Princesa, Palawan, Philippines|Boehringer Ingelheim Investigational Site 26, Quezon City, Philippines|Boehringer Ingelheim Investigational Site 11, Rosales, Pangasinan, Philippines|Boehringer Ingelheim Investigational Site 21, San Fernando, La Union, Philippines|Boehringer Ingelheim Investigational Site 9, San Fernando, Pampanga, Philippines|Boehringer Ingelheim Investigational Site 13, San Jose, Nueva Ecija, Philippines|Boehringer Ingelheim Investigational Site 29, San Juan, Philippines|Boehringer Ingelheim Investigational Site 8, San Pablo, Laguna, Philippines|Boehringer Ingelheim Investigational Site 50, San Pedro, Laguna, Philippines|Boehringer Ingelheim Investigational Site 41, Santiago city, Isabela, Philippines|Boehringer Ingelheim Investigational Site 36, Sogod, Southern Leyte, Philippines|Boehringer Ingelheim Investigational Site 38, Sta.Maria, Bulacan, Philippines|Boehringer Ingelheim Investigational Site 6, Tacloban, Philippines|Boehringer Ingelheim Investigational Site 33, Tagbilaran, Bohol, Philippines|Boehringer Ingelheim Investigational Site 14, Tuguegarao, Cagayan, Philippines|Boehringer Ingelheim Investigational Site 18, Urdaneta, Pangasinan, Philippines|Boehringer Ingelheim Investigational Site 46, Valencia City Bukidnon, Philippines|Boehringer Ingelheim Investigational Site 17, Valenzuela, Bulacan, Philippines|Boehringer Ingelheim Investigational Site 22, Zamboanga, Philippines Less <<
NCT02004366 Type 2 Diabetes Phase 4 Completed - United States, Colorado ... More >> University of Colorado Denver, Colorado, United States, 80220 United States, Georgia Emory University Hospital Atlanta, Georgia, United States, 30322 Grady Memorial Hospital Atlanta, Georgia, United States United States, Illinois Rush University Medical Center Chicago, Illinois, United States, 60612 United States, Massachusetts Boston Medical Center Boston, Massachusetts, United States, 02118 Less <<
NCT00935220 Diabetes Mellitus, Type 2 Phase 1 Completed - United States, California ... More >> 1218.55.0006 Boehringer Ingelheim Investigational Site Cypress, California, United States United States, Florida 1218.55.0008 Boehringer Ingelheim Investigational Site Deland, Florida, United States 1218.55.0004 Boehringer Ingelheim Investigational Site Miami, Florida, United States United States, Maryland 1218.55.0005 Boehringer Ingelheim Investigational Site Baltimore, Maryland, United States United States, New York 1218.55.0003 Boehringer Ingelheim Investigational Site New York, New York, United States United States, Texas 1218.55.0001 Boehringer Ingelheim Investigational Site Dallas, Texas, United States Less <<
NCT02004366 - Completed - -
NCT00935220 - Completed - -
NCT02240680 - Completed - -
NCT01943019 Schizophrenia PHASE1 TERMINATED 2025-08-18 Pusat Perubatan Universiti Keb... More >>angsaan Malaysia, Bandar Tun Razak, Kuala Lumpur, 56000, Malaysia Less <<
NCT03011177 Type2 Diabetes Mellitus Phase 4 Recruiting April 2019 Korea, Republic of ... More >> Asan Medical Center Recruiting Seoul, Korea, Republic of Contact: JY Park    82216887575 Less <<
NCT02429232 Osteoporosis ... More >>Diabetes Mellitus Less << Phase 4 Unknown December 2017 -
NCT03429543 Diabetes Mellitus, Type 2 Phase 3 Recruiting January 31, 2022 -
NCT03667300 Type2 Diabetes Mellitus ... More >> Albuminuria Renal Insufficiency Less << Phase 2 Enrolling by invitation January 31, 2019 Korea, Republic of ... More >> Samsung Medical Center Seoul, Korea, Republic of, 135-710 Less <<
NCT02084082 - Completed - -
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NCT02121509 Healthy Phase 1 Completed - Germany ... More >> 1288.10.1 Boehringer Ingelheim Investigational Site Ingelheim, Germany Less <<
NCT02121509 - Completed - -
NCT01540487 Healthy Phase 1 Completed - China ... More >> 1288.5.86001 Boehringer Ingelheim Investigational Site Beijing, China Less <<
NCT02084056 - Completed - -
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NCT01540487 - Completed - -
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NCT03051243 DM2 Phase 3 Not yet recruiting November 1, 2019 -
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NCT02372630 Type 2 Diabetes Phase 4 Active, not recruiting May 2018 United States, New York ... More >> ECMC Ambulatory Center, 3rd Floor Buffalo, New York, United States, 14215 Less <<
NCT03338803 Diabetes Mellitus, Type 2 COMPLETED 2018-02-02 Optum, Eden Prairie, Minnesota... More >>, 55344, United States Less <<
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NCT02280174 Type 2 Diabetes Phase 4 Unknown October 2016 Argentina ... More >> National University of Formosa Recruiting Formosa, Argentina, 3600 Contact: Juan Pa Nogueira, MD/PhD    00543704425447    nogueirajuanpatricio@gmail.com Less <<
NCT02097342 Type 2 Diabetes Mellitus ... More >> Insulin Sensitivity/Resistance Less << Phase 4 Unknown January 2015 India ... More >> Postgraduate Institute of Medical Education & Research Recruiting Chandigarh, India, 160012 Contact: Anil Bhansali, MD DM       anilbhansaliendocrine@gmail.com Less <<
NCT02752113 Diabetes Mellitus Type 2 Phase 3 Recruiting January 2019 Germany ... More >> Clinical Research Center, Dept of Nephrology and Hypertenison, University of Erlangen/Nürnberg Recruiting Erlangen, Bavaria, Germany, 91054 Contact: Christian Ott, MD    +49-9131-85 ext 36245    christian.ott@uk-erlangen.de    Contact: Roland Schmieder, Prof. MD    +49 9131 85 ext 36245    roland.schmieder@uk-erlangen.de    Principal Investigator: Roland Schmieder, Prof. MD          Sub-Investigator: Christian Ott, MD Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.58mL

2.12mL

1.06mL

21.16mL

4.23mL

2.12mL

References

[1]Thomas L, Eckhardt M, et al.(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82.

[2]Eckhardt M, Langkopf E, et al. 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. J Med Chem. 2007 Dec 27;50(26):6450-3.

[3]Sortino MA, Sinagra T, et al. Linagliptin: A thorough Characterization beyond Its Clinical Efficacy. Front Endocrinol (Lausanne). 2013 Feb 26;4:16.

[4]Kern M, Klöting N, et al. Linagliptin improves insulin sensitivity and hepatic steatosis in diet-induced obesity. PLoS One. 2012;7(6):e38744.

[5]Linagliptin

[7]Linagliptin inhibits lipopolysaccharide-stimulated interleukin-6 production, intranuclear p65 expression, and p38 mitogen-activated protein kinase phosphorylation in human umbilical vein endothelial cells

[8]Syam YM, El-Karim SSA, Nasr T, Elseginy SA, Anwar MM, Kamel MM, Ali HF. Design, Synthesis and Biological Evaluation of Spiro Cyclohexane-1,2- Quinazoline Derivatives as Potent Dipeptidyl Peptidase IV Inhibitors. Mini Rev Med Chem. 2019;19(3):250-269. doi: 10.2174/1389557517666170828121018. PMID: 28847268.

[9]Miglio G, Vitarelli G, Klein T, Benetti E. Effects of linagliptin on human immortalized podocytes: a cellular system to study dipeptidyl-peptidase 4 inhibition. Br J Pharmacol. 2017 May;174(9):809-821. doi: 10.1111/bph.13739. Epub 2017 Mar 6. PMID: 28177527; PMCID: PMC5386990.

[10]Kanasaki K, Shi S, Kanasaki M, He J, Nagai T, Nakamura Y, Ishigaki Y, Kitada M, Srivastava SP, Koya D. Linagliptin-mediated DPP-4 inhibition ameliorates kidney fibrosis in streptozotocin-induced diabetic mice by inhibiting endothelial-to-mesenchymal transition in a therapeutic regimen. Diabetes. 2014 Jun;63(6):2120-31. doi: 10.2337/db13-1029. Epub 2014 Feb 26. PMID: 24574044.

[11]Manrique C, Habibi J, Aroor AR, Sowers JR, Jia G, Hayden MR, Garro M, Martinez-Lemus LA, Ramirez-Perez FI, Klein T, Meininger GA, DeMarco VG. Dipeptidyl peptidase-4 inhibition with linagliptin prevents western diet-induced vascular abnormalities in female mice. Cardiovasc Diabetol. 2016 Jul 8;15:94. doi: 10.1186/s12933-016-0414-5. PMID: 27391040; PMCID: PMC4938903.

[12]Darsalia V, Ortsäter H, Olverling A, Darlöf E, Wolbert P, Nyström T, Klein T, Sjöholm Å, Patrone C. The DPP-4 inhibitor linagliptin counteracts stroke in the normal and diabetic mouse brain: a comparison with glimepiride. Diabetes. 2013 Apr;62(4):1289-96. doi: 10.2337/db12-0988. Epub 2012 Dec 3. PMID: 23209191; PMCID: PMC3609599.

 

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