Structure of Varespladib
CAS No.: 172732-68-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Varespladib is a potent and selective human non-pancreatic secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM.
Synonyms: LY315920
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 172732-68-2 |
Formula : | C21H20N2O5 |
M.W : | 380.39 |
SMILES Code : | CCC1=C(C2=C(C=CC=C2N1CC3=CC=CC=C3)OCC(O)=O)C(C(N)=O)=O |
Synonyms : |
LY315920
|
MDL No. : | MFCD00944812 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Description |
Varespladib (LY315920) is a potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2) with an IC50 of 9 nM. It significantly inhibits sPLA2 activity in serum from various species, including rats, rabbits, guinea pigs, and humans, with IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively[1].
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In Vitro:
Concentration | Treated Time | Description | References |
HaCaT cells | 256 µM | 24 h | To test the inhibitory effect of Varespladib on the cytotoxicity of D. russelii and B. asper venoms, results showed no inhibition | PMC10721902 |
HaCaT cells | 128 µM | 24 h | To test the inhibitory effect of Varespladib on the cytotoxicity of various snake venoms, results showed no inhibition on any of the six tested venoms | PMC10721902 |
HaCaT cells | 22.9 μg/mL | 24 h | To evaluate the inhibitory effect of Varespladib on cytotoxicity induced by snake venom. Results showed that Varespladib significantly reduced the cytotoxicity of crude venom but had no significant effect on the purified CTx combination. | PMC11087757 |
Rat citrated plasma | 1 mM | 30 min | Varespladib alone significantly prevented the venom-induced procoagulant action for PT, with approximately 16.4% of decreasing being verified | PMC8790531 |
In Vivo:
Administration | Dosage | Frequency | Description | References |
Mice | Snake venom-induced dermonecrosis model | Intradermal injection | 19 µg | Single dose, duration of 72 hours | To test the inhibitory effect of Varespladib on dermonecrosis induced by B. asper and C. atrox venoms, results showed significant reduction in lesion area | PMC10721902 |
Mice | Snake venom-induced dermonecrosis model | Intradermal injection | 19 μg | Single injection, lasting 72 hours | To evaluate the inhibitory effect of Varespladib on dermonecrosis induced by snake venom. Results showed that Varespladib significantly reduced dermonecrosis caused by East and West African N. nigricollis and N. pallida venoms. | PMC11087757 |
Mice | Snake envenoming model | Intravenous injection | 60 µg | Single dose, monitored for 6 hours | To test the efficacy of Varespladib as a solo therapy in preventing lethality caused by snake venom, results showed that Varespladib failed to fully prevent lethality but prolonged survival time. | PMC7738508 |
Mouse | Mmp2-/- mice | Oral | 10 mg/kg | Once daily for 2 days | To investigate the effect of Varespladib on sPLA2 activity and inflammatory response in MMP-2 deficient mice, results showed that Varespladib significantly reduced sPLA2 activity and inflammatory response. | PMC4579961 |
Mice | ApoE2/2 mice | Dietary supplementation | 15 mg/kg or 150 mg/kg | Once daily for 12 weeks | To evaluate the effects of A-002 alone or in combination with pravastatin on atherosclerosis, lipids, and paraoxonase (PON) activity. A-002 significantly reduced atherosclerotic lesion area, increased fibrous cap size, and elevated HDL levels and plasma PON activity. | PMC2656655 |
Wistar rats | Subcutaneous hemorrhage model | Intraperitoneal injection | 1 mM | Single injection, 24-hour monitoring | Varespladib alone or associated with antivenom exhibited a mild protective effect on the venom-induced subcutaneous haemorrhage | PMC8790531 |
Mice | Mmp9-/- mice | Oral gavage | 10 mg/kg | Once daily for 5 days | To determine the contribution of systemic sPLA2 to the lipid metabolic phenotype of MMP-9 deficiency. Varespladib partially restored the hepatic transcriptional responses to dietary cholesterol in MMP-9-deficient mice. | PMC5121519 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT02218125 | Healthy | Phase 1 | Completed | - | United States, Massachusetts ... More >> Boston, Massachusetts, United States Less << |
NCT00522197 | Lung Cancer P... More >>recancerous Condition Less << | Phase 2 | Completed | - | - |
NCT03614221 | Atopic Dermatitis | Phase 2 | Not yet recruiting | July 31, 2021 | Taiwan ... More >> Taipei Chang Gung Memorial Hospital Not yet recruiting Taipei, Taiwan, 10507 Contact: Yin-Ku Lin, MD., PhD. 886-2-24311311 ext 2127 lin1266@cgmh.org.tw Principal Investigator: Yin-Ku Lin, MD., PhD. Sub-Investigator: Chun-Bing Chen, MD. Sub-Investigator: Chin-Yi Yang, MD. Sub-Investigator: Chun-Wei Lu, MD. Sub-Investigator: Wen-Hung Chung, MD., PhD. Sub-Investigator: Chih-Yung Chiu, MD., PhD Sub-Investigator: Shih-Chi Su, PhD. Sub-Investigator: Lai-Chu See, PhD. Linkou Chang Gung Memorial Hospital Not yet recruiting Taoyuan, Taiwan, 33305 Contact: Yin-Ku Lin, MD., PhD 886-2-241-3131 ext 2127 lin1266@cgmh.org.tw Principal Investigator: Yin-Ku Lin, MD., PhD Sub-Investigator: Chun-Bing Chen, MD. Sub-Investigator: Chin-Yi Yang, MD. Sub-Investigator: Chun-Wei Lu, MD. Sub-Investigator: Wen-Hung Chung, MD., PhD Sub-Investigator: Chih-Yung Chu, MD., PhD Sub-Investigator: Shih-Chi Su, PhD. Sub-Investigator: Lai-Chu See, PhD. Less << |
NCT01536288 | Acute Mountain Sickness ... More >> Environmental Illness Less << | Phase 2 | Completed | - | Taiwan ... More >> Dept of Emergency medicine, Chang Gung Memorial Hospital Kweishan, Taoyuan, Taiwan, 333 Less << |
NCT00839176 | Major Depressive Disorder (MDD... More >>) Less << | Phase 2 | Completed | - | United States, Colorado ... More >> Denver, Colorado, United States, 80239 United States, Georgia Atlanta, Georgia, United States, 30308 United States, Maryland Rockville, Maryland, United States, 20852 Less << |
NCT00606879 | Advanced Cancer | Phase 1 | Terminated | June 2009 | United States, California ... More >> Premier Onocology, California Santa Monica, California, United States, 90404 United States, Tennessee Sarah Cannon Research Institute Nashville, Tennessee, United States, 37203 Less << |
NCT00359294 | Solid Tumors ... More >>Lymphoma Less << | Phase 1 | Terminated(Considered not nece... More >>ssary to continue with this trial; recommended dose was reached in other phase I trials) Less << | September 2008 | United States, Pennsylvania ... More >> Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111-2497 Less << |
NCT01157104 | Chronic Hepatitis C | Phase 1 | Completed | - | - |
NCT02572089 | Drug Overdose ... More >> Opioid-Related Disorders Less << | Phase 1 | Completed | - | United States, Kansas ... More >> Vince Associates Clinical Research Overland Park, Kansas, United States, 66212 Less << |
NCT01299636 | Solid Tumors | Phase 1 | Completed | - | United States, Texas ... More >> START- South Texas Accelerated Research Therapeutics, LLC San Antonio, Texas, United States, 78229 Less << |
NCT02750748 | Opioid-Related Disorders | Phase 1 | Completed | - | United States, Kansas ... More >> Vince and Associates Clinical Research, Inc. Overland Park, Kansas, United States, 66212 Less << |
NCT01332695 | Essential Tremor | Phase 2 | Completed | - | United States, California ... More >> Los Angeles, California, United States Less << |
NCT02661581 | Diabetes | Not Applicable | Unknown | September 2017 | Canada, British Columbia ... More >> St. Paul's Hospital Vancouver, British Columbia, Canada, V6Z 1Y6 Less << |
NCT02930889 | Benign Prostatic Hyperplasia | Not Applicable | Recruiting | October 2021 | United States, Minnesota ... More >> University of Minnesota Recruiting Minneapolis, Minnesota, United States, 55455 Contact: Shamar J Young, MD 612-626-5388 youn1862@umn.edu Contact: Jafar Golzarian, MD 612-626-5388 jafar@umn.edu Principal Investigator: Jafar Golzarian, MD Sub-Investigator: Shamar Young, MD Less << |
NCT01303510 | Influenza | Phase 4 | Completed | - | Switzerland ... More >> Covance Clinical Research Unit AG Allschwil, Switzerland, 4123 Less << |
NCT01303510 | - | Completed | - | - | |
NCT01349283 | Hepatitis B | Phase 3 | Completed | - | China, Jiangsu ... More >> Center for Disease Control and Prevention Jiangsu Province Nanjing, Jiangsu, China Less << |
NCT01412281 | Influenza | Phase 3 | Completed | - | Switzerland ... More >> Covance Clinical Research Unit AG Allschwil, Switzerland, 4123 Less << |
NCT01412281 | - | Completed | - | - | |
NCT01786135 | Burkitt Lymphoma ... More >> Lymphoma, Follicular Lymphoma, Large B-Cell, Diffuse Lymphoma, Mantle-Cell Precursor B-cell Lymphoblastic Leukemia-Lymphoma Less << | Phase 1 | Completed | - | United States, Alabama ... More >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35294 United States, California City of Hope National Medical Center Duarte, California, United States, 91010-3000 Stanford Cancer Center Stanford, California, United States, 94305 United States, Florida H. Lee Moffitt Cancer Center & Research Institute Tampa, Florida, United States, 33612 United States, New York Memorial Sloan Kettering Cancer Center New York, New York, United States, 10021 United States, Texas MD Anderson Cancer Center / University of Texas Houston, Texas, United States, 77030-4095 Less << |
NCT02326584 | Acute Myeloid Leukemia ... More >> Acute Myelogenous Leukemia Less << | Phase 1 | Completed | - | United States, Alabama ... More >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35294 United States, California City of Hope National Medical Center Duarte, California, United States, 91010-3000 United States, Colorado Colorado Blood Cancer Institute Denver, Colorado, United States, 80218 United States, Illinois Cardinal Bernardin Cancer Center / Loyola University Medical Center Maywood, Illinois, United States, 60153 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 United States, Michigan Karmanos Cancer Institute / Wayne State University Detroit, Michigan, United States, 48201 United States, New Jersey Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 United States, Ohio Cleveland Clinic, The Cleveland, Ohio, United States, 44195 James Cancer Hospital / Ohio State University Columbus, Ohio, United States, 43210 United States, Tennessee Sarah Cannon Research Institute Nashville, Tennessee, United States, 30384 United States, Texas Charles A. Sammons Cancer Center / Baylor University Medical Center Dallas, Texas, United States, 75246 MD Anderson Cancer Center / University of Texas Houston, Texas, United States, 77030-4095 United States, Washington Fred Hutchinson Cancer Research Center Seattle, Washington, United States, 98109-1024 Less << |
NCT00862992 | Schizophrenia | Phase 2 | Completed | - | Japan ... More >> Hoyu Hospital Kure-City, Hiroshima-ken, Japan Less << |
NCT03434210 | Schizophrenia | Not Applicable | Not yet recruiting | October 2019 | - |
NCT00888446 | Human Immunodeficiency Virus I... More >>nfections HIV Infections Less << | Phase 2 | Completed | - | South Africa ... More >> Desmond Tutu HIV Centre Cape Town Cape Town, South Africa, 7920 Medunsa South Africa, South Africa, 0204 Perinatal HIV Research Unit, Baragwanath Hospital Soweto, South Africa, 2013 Uganda Uganda Virus Research Institute Entebbe, Uganda Zambia Zambia-Emory HIV Research Project (ZEHRP) Lusaka, Zambia Less << |
NCT01626859 | Schizophrenia | Phase 2 Phase 3 | Completed | - | Japan ... More >> Sakai, Osaka, Japan Less << |
NCT01625000 | Schizophrenia | Phase 2 Phase 3 | Completed | - | Japan ... More >> Sapporo, Hokkaido, Japan Korea, Republic of Seoul, Korea, Republic of Taiwan Taipei, Taiwan Less << |
NCT01625897 | Schizophrenia | Phase 2 Phase 3 | Completed | - | Japan ... More >> Aizuwakamatsu, Fukushima, Japan Less << |
NCT01626885 | Schizophrenia | Phase 2 Phase 3 | Completed | - | Japan ... More >> Kurayoshi, Tottori, Japan Less << |
NCT01350037 | Biliary Tract Diseases ... More >> Pancreatic Diseases Less << | Phase 4 | Completed | - | Finland ... More >> Helsiki University Central Hospital,Meilahti Hospital,Endoscopy unit Helsinki, Uusimaa, Finland, 00029 Less << |
NCT01626872 | Schizophrenia | Phase 2 Phase 3 | Completed | - | Japan ... More >> Sapporo, Hokkaido, Japan Korea, Republic of Seoul, Korea, Republic of Taiwan Taipei, Taiwan Less << |
NCT00945282 | Infection, Human Immunodeficie... More >>ncy Virus Less << | Phase 2 | Completed | - | Argentina ... More >> GSK Investigational Site Buenos Aires, Argentina, B1602DBG Less << |
NCT00434473 | Sickle Cell Disease ... More >> Vaso-occlusive Crisis Acute Chest Syndrome Less << | Phase 2 | Completed | - | United States, District of Col... More >>umbia Howard University Hospital Washington, District of Columbia, United States, 20060 United States, Georgia Children's Healthcare of Atlanta Atlanta, Georgia, United States, 30342 United States, Illinois Children's Memorial Hospital Chicago, Illinois, United States, 60614 United States, New York SUNY Downstate Medical Center Brooklyn, New York, United States, 11203 United States, North Carolina Duke University Comprehensive Sickle Cell Center Durham, North Carolina, United States, 27713 United States, Virginia Virginia Commonwealth University Richmond, Virginia, United States, 23219 Less << |
NCT00429923 | Inflammation | Phase 3 | Completed | - | United States, Missouri ... More >> Comprehensive Eye Care Washington, Missouri, United States, 63090 Less << |
NCT00429923 | - | Completed | - | - | |
NCT00945282 | - | Completed | - | - | |
NCT00430092 | Inflammation | Phase 3 | Completed | - | United States, Missouri ... More >> Comprehensive Eye Care Washington, Missouri, United States, 63090 Less << |
NCT00430092 | - | Completed | - | - | |
NCT01513239 | Clostridium Difficile Infectio... More >>n Less << | Phase 3 | Completed | - | - |
NCT01314599 | Acute Leukemia | Phase 1 | Completed | - | United States, Minnesota ... More >> Rochester, Minnesota, United States, 55905 United States, Texas Houston, Texas, United States, 77030 Less << |
NCT00455546 | Coronary Artery Disease (CAD) | Phase 2 | Completed | - | - |
NCT03588559 | Blood Pressure | Not Applicable | Completed | - | United States, Colorado ... More >> Clinimark, LLC Louisville, Colorado, United States, 80027 Less << |
NCT03692221 | Disc Degeneration | Early Phase 1 | Not yet recruiting | September 30, 2022 | United States, Ohio ... More >> University Hospitals Cleveland Medical Center Not yet recruiting Cleveland, Ohio, United States, 44106 Contact: Mario A Becerra, RN, BA 216-844-1734 Mario.Becerra@UHhospitals.org Principal Investigator: Melinda Lawrence, MD Sub-Investigator: Salim Hayek, MD Sub-Investigator: Zhenghong Lee, PhD Sub-Investigator: Ameya Nayate, MD Sub-Investigator: Jane Reese-Koc, BA, MBA Sub-Investigator: Sidhartha Tavri, MD Sub-Investigator: Elias Veizi, MD, PhD Less << |
NCT00525954 | Coronary Artery Disease | Phase 2 | Completed | - | United States, Alabama ... More >> Mobile Heart Specialists Mobile, Alabama, United States, 36608 United States, Arizona Sonoran Health Specialists Scottsdale, Arizona, United States, 85260 United States, Florida Pasco Cardiology Center Hudson, Florida, United States, 34667 Charlotte Cardiovascular Institute Port Charlotte, Florida, United States, 33952 Florida Cardiovascular Research Institute Tampa, Florida, United States, 33609 United States, Georgia Augusta Cardiology Clinic Augusta, Georgia, United States, 30901 United States, Kentucky Louisville Cardiology Medical Group Louisville, Kentucky, United States, 40207 United States, Maine Maine Research Associates Auburn, Maine, United States, 04210 United States, New York United Medical Associates Binghamton, New York, United States, 13901 Cardiology PC Syracuse, New York, United States, 13210 United States, Texas Austin Heart Austin, Texas, United States, 78705 United States, Virginia Clinical Research Associates of Tidewater Norfolk, Virginia, United States, 23507 United States, Wisconsin Wisconsin Heart, SC Madison, Wisconsin, United States, 53715 Less << |
NCT00743925 | Acute Coronary Syndrome | Phase 2 | Completed | - | Georgia ... More >> Cardiological hospital of The Patriarchate of all Georgia Tbilisi, Georgia, 0102 Tbilisi State Medical University, Al. Aladashvili University Clinic Tbilisi, Georgia, 0102 Cardio Reanimation Centre Tbilisi, Georgia, 0141 Cardiological Clinic "Guli" Tbilisi, Georgia, 0144 Tbilisi LTD Cardiology Clinic Tbilisi, Georgia, 0144 Emergency Cardiology Center by acad. G. Chapidze Tbilisi, Georgia, 0159 National Center of Therapy Tbilisi, Georgia, 0159 Multiprofile Clinical Hospital of Tbilisi #2 Tbilisi, Georgia, 0164 Diagnostic Services Clinic Tbilisi, Georgia, 0179 Limited Company "ADAPTI" The Clinic of Angiocardiology "ADAPTI" Tbilisi, Georgia, 0186 Russian Federation New Hospital Medical Union Ekaterinburg, Russian Federation, 620109 Municipal Healthcare Institution Gatchina, Russian Federation, 188300 Municipal Healthcare Institution Kemerovo, Russian Federation, 650002 Non-State Healthcare Institution Kemerovo, Russian Federation, 650055 Krasnoyarsk Medical Academy Krasnoyarsk, Russian Federation, 660022 State Healthcare Intstitution of Moscow Moscow, Russian Federation, 111539 City Clinical Hospital №12 Nizhniy Novgorod, Russian Federation, 603003 Municipal Healthcare Institution Novosibirsk, Russian Federation, 630008 Regional State Healthcare Institution Novosibirsk, Russian Federation, 630047 Municipal Healthcare Institution Perm, Russian Federation, 614107 St.Petersburg State Healthcare Institution Saint-Petersburg, Russian Federation, 190000 St.Petersburg State Healthcare Institution Saint-Petersburg, Russian Federation, 191144 Saint-Petersburg State Healthcare Institution Saint-Petersburg, Russian Federation, 198205 St.Petersburg State Healthcare Institution Saint-Petersburg, Russian Federation, 199106 State Healthcare Institution Samara, Russian Federation, 443070 Saratov State Medical University Saratov, Russian Federation, 410012 Federal State Institution Saratov, Russian Federation, 410028 State Healthcare Institution St-Petersburg, Russian Federation, 195197 St.Petersburg State Healthcare Institution St-Petersburg, Russian Federation, 195257 State Educational Institution for Further Professional Training St.Petersburg, Russian Federation, 191015 Federal State Healthcare Institution St.Petersburg, Russian Federation, 194044 State Institution Research Cardiology Institute Tomsk, Russian Federation, 634012 Tyumen Cardiology Center, Tyumen, Russian Federation, 625026 Ukraine Municipal Clinical Hospital No. 27 Kharkiv, Ukraine, 61002 Department of Cardiology of Central Clinical Hospital Kharkiv, Ukraine, 61018 L.T. Malaya Institute of Therapy of AMS of Ukraine Kharkiv, Ukraine, 61039 Kharkiv Medical Academy of Post-Graduate Education Kharkiv, Ukraine, 61178 Kyiv City Clinical Hospital #1 Kyiv, Ukraine, 02175 National Scientific Center Kyiv, Ukraine, 03680 Lviv Danylo Halytsky National University Lviv, Ukraine, 79000 Lviv Regional State Clinical Treatment and Diagnostics Cardiology Center Lviv, Ukraine, 79015 Uzhgorod National University Uzhgorod, Ukraine, 88014 Zaporizhzhya Regional Cardiological Dispensary Zaporizhzhya, Ukraine, 69000 Zhytomyr city hospital #1 Zhytomyr, Ukraine, 10002 Less << |
NCT01130246 | Acute Coronary Syndrome | Phase 3 | Terminated(Lack of efficacy) | - | - |
NCT00533039 | Coronary Artery Disease | Phase 2 | Completed | - | Canada, Ontario ... More >> Toronto General Hospital Toronto, Ontario, Canada, M5G 2C4 Less << |
NCT01522196 | Sickle Cell Disease ... More >> Vaso-occlusive Crisis Less << | Phase 2 | Terminated(change in company p... More >>lans) Less << | - | United States, Georgia ... More >> Investigator Site 101 Atlanta, Georgia, United States, 30342 Less << |
NCT01513239 | - | Completed | - | - | |
NCT01359579 | Renal Impairment | Phase 1 | Terminated(Lack of efficacy) | June 2012 | United States, Florida ... More >> Investigator Site 101 Orlando, Florida, United States, 32809 United States, Minnesota Investigator Site 102 Minneapolis, Minnesota, United States, 55404 United States, Tennessee Investigator Site 103 Knoxville, Tennessee, United States, 37920 Less << |
NCT01359605 | Healthy Volunteers | Phase 1 | Completed | - | United States, Nebraska ... More >> Celerion Lincoln, Nebraska, United States, 68502 Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.63mL 0.53mL 0.26mL |
13.14mL 2.63mL 1.31mL |
26.29mL 5.26mL 2.63mL |