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Chemical Structure| 172732-68-2 Chemical Structure| 172732-68-2

Structure of Varespladib
CAS No.: 172732-68-2

Chemical Structure| 172732-68-2

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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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Product Details of Varespladib

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

Safety of Varespladib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

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].

In Vitro:

Cell Line
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:

Species
Animal Model
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 <<

Protocol

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

References

 

Historical Records

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