Varespladib Methyl

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MedKoo CAT#: 326901

CAS#: 172733-08-3

Description: Varespladib Methyl (A-002; LY-333013; S-3013) is a secretory phospholipase A2 (sPLA2) inhibitor as a potential treatment for acute coronary syndrome (ACS). Varespladib methyl is an orally bioavailable prodrug of the molecule varespladib. Varespladib inhibits the IIA, V and X isoforms of sPLA2 to reduce inflammation, lower and modulate lipid levels, and reduce levels of C-reactive protein (CRP) and interleukin-6 (IL-6), both indicators of inflammation.


Chemical Structure

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Varespladib Methyl
CAS# 172733-08-3

Theoretical Analysis

MedKoo Cat#: 326901
Name: Varespladib Methyl
CAS#: 172733-08-3
Chemical Formula: C22H22N2O5
Exact Mass: 394.1529
Molecular Weight: 394.427
Elemental Analysis: C, 66.99; H, 5.62; N, 7.10; O, 20.28

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: A-002; A002; A002; LY-333013; LY 333013; LY333013; S-3013; S 3013; S3013; Varespladib Methyl

IUPAC/Chemical Name: methyl 2-((3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yl)oxy)acetate

InChi Key: VJYDOJXJUCJUHL-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H22N2O5/c1-3-15-20(21(26)22(23)27)19-16(24(15)12-14-8-5-4-6-9-14)10-7-11-17(19)29-13-18(25)28-2/h4-11H,3,12-13H2,1-2H3,(H2,23,27)

SMILES Code: O=C(OC)COC1=CC=CC2=C1C(C(C(N)=O)=O)=C(CC)N2CC3=CC=CC=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 394.427 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Varespladib. Am J Cardiovasc Drugs. 2011;11(2):137-43. doi: 10.2165/11533650-000000000-00000. Review. PubMed PMID: 21446779.

2: Rosenson RS, Fraser H, Goulder MA, Hislop C. Anti-inflammatory effects of varespladib methyl in diabetic patients with acute coronary syndrome. Cardiovasc Drugs Ther. 2011 Dec;25(6):539-44. doi: 10.1007/s10557-011-6344-2. PubMed PMID: 21989792.

3: Karakas M, Koenig W. Varespladib methyl, an oral phospholipase A2 inhibitor for the potential treatment of coronary artery disease. IDrugs. 2009 Sep;12(9):585-92. PubMed PMID: 19697278.

4: Rosenson RS. After FRANCIS: next steps in the clinical evaluation of varespladib methyl. Future Cardiol. 2011 Jan;7(1):11-8. doi: 10.2217/fca.10.118. PubMed PMID: 21174506.

5: Rosenson RS, Fraser H, Trias J, Hislop C. Varespladib methyl in cardiovascular disease. Expert Opin Investig Drugs. 2010 Oct;19(10):1245-55. doi: 10.1517/13543784.2010.517193. Review. PubMed PMID: 20809869.

6: Arsenault BJ, Boekholdt SM, Kastelein JJ. Varespladib: targeting the inflammatory face of atherosclerosis. Eur Heart J. 2011 Apr;32(8):923-6. doi: 10.1093/eurheartj/ehq385. Epub 2010 Nov 25. PubMed PMID: 21112895.

7: Rosenson RS, Elliott M, Stasiv Y, Hislop C; PLASMA II Investigators. Randomized trial of an inhibitor of secretory phospholipase A2 on atherogenic lipoprotein subclasses in statin-treated patients with coronary heart disease. Eur Heart J. 2011 Apr;32(8):999-1005. doi: 10.1093/eurheartj/ehq374. Epub 2010 Nov 16. PubMed PMID: 21081550.

8: Rosenson RS, Hislop C, Elliott M, Stasiv Y, Goulder M, Waters D. Effects of varespladib methyl on biomarkers and major cardiovascular events in acute coronary syndrome patients. J Am Coll Cardiol. 2010 Sep 28;56(14):1079-88. doi: 10.1016/j.jacc.2010.06.015. Erratum in: J Am Coll Cardiol. 2011 Mar 29;57(13):1501. PubMed PMID: 20863951.

9: Nicholls SJ, Cavender MA, Kastelein JJ, Schwartz G, Waters DD, Rosenson RS, Bash D, Hislop C. Inhibition of secretory phospholipase A(2) in patients with acute coronary syndromes: rationale and design of the vascular inflammation suppression to treat acute coronary syndrome for 16 weeks (VISTA-16) trial. Cardiovasc Drugs Ther. 2012 Feb;26(1):71-5. doi: 10.1007/s10557-011-6358-9. PubMed PMID: 22109255.

10: Rosenson RS, Hurt-Camejo E. Phospholipase A2 enzymes and the risk of atherosclerosis. Eur Heart J. 2012 Dec;33(23):2899-909. doi: 10.1093/eurheartj/ehs148. Epub 2012 Jul 15. Review. PubMed PMID: 22802388.

11: Guo Y, Li B, Xu X, Wu R, Li W. sPLA2-IIA Augments Oxidized LDL-Induced MCP-1 Expression in Vitro Through Activation of Akt. Cell Physiol Biochem. 2015;37(4):1345-54. doi: 10.1159/000430255. Epub 2015 Oct 22. PubMed PMID: 26488172.

12: Rosenson RS. Phospholipase A2 inhibition and atherosclerotic vascular disease: prospects for targeting secretory and lipoprotein-associated phospholipase A2 enzymes. Curr Opin Lipidol. 2010 Dec;21(6):473-80. doi: 10.1097/MOL.0b013e32833eb581. Review. PubMed PMID: 20739882.

13: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Sep;31(7):463-93. PubMed PMID: 19907722.