Varespladib
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MedKoo CAT#: 522365

CAS#: 172732-68-2

Description: Varespladib, aslo known as LY315920, is a secreted phospholipase A2 (sPLA2) inhibitor (IC50 = 50 - 750 nM for a range of sPLA2 isoforms). Varespladib reduces atherosclerosis and aneurysm formation in ApoE-/- mice and in guinea pigs. Varespladib significantly reduces the post-ACS inflammatory response in those with and without diabetes. Varespladib may be potentially useful for treatment of coronary artery disease.


Price and Availability

Size Price Shipping out time Quantity
5mg USD 90 Same day
10mg USD 150 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 750 Same day
200mg USD 1250 Same day
500mg USD 2050 2-3 months
1g USD 3850 2-3 months
2g USD 6450 2-3 months
Inquire bulk and customized quantity

Pricing updated 2020-07-06. Prices are subject to change without notice.

Varespladib (LY315920), purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 522365
Name: Varespladib
CAS#: 172732-68-2
Chemical Formula: C21H20N2O5
Exact Mass: 380.13722
Molecular Weight: 380.4
Elemental Analysis: C, 66.31; H, 5.30; N, 7.36; O, 21.03


Synonym: LY315920; LY-315920; LY 315920; A-002; A002; A 002; Varespladib

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

InChi Key: BHLXTPHDSZUFHR-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H20N2O5/c1-2-14-19(20(26)21(22)27)18-15(9-6-10-16(18)28-12-17(24)25)23(14)11-13-7-4-3-5-8-13/h3-10H,2,11-12H2,1H3,(H2,22,27)(H,24,25)

SMILES Code: NC(C(C1=C(CC)N(CC2=CC=CC=C2)C3=C1C(OCC(O)=O)=CC=C3)=O)=O


Technical Data

Appearance:
White to beige solid powder

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

Certificate of Analysis:

Safety Data Sheet (SDS):

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, not in water

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


References

1: Nicholls SJ, Kastelein JJ, Schwartz GG, Bash D, Rosenson RS, Cavender MA, Brennan DM, Koenig W, Jukema JW, Nambi V, Wright RS, Menon V, Lincoff AM, Nissen SE; VISTA-16 Investigators. Varespladib and cardiovascular events in patients with an acute coronary syndrome: the VISTA-16 randomized clinical trial. JAMA. 2014 Jan 15;311(3):252-62. doi: 10.1001/jama.2013.282836. PubMed PMID: 24247616.

2: De Luca D, Vendittelli F, Trias J, Fraser H, Minucci A, Gentile L, Perez-Gil J, Conti G, Antonelli M, Capoluongo ED. Surfactant and varespladib co-administration in stimulated rat alveolar macrophages culture. Curr Pharm Biotechnol. 2013;14(4):445-8. PubMed PMID: 23590147.

3: De Luca D, Minucci A, Piastra M, Cogo PE, Vendittelli F, Marzano L, Gentile L, Giardina B, Conti G, Capoluongo ED. Ex vivo effect of varespladib on secretory phospholipase A2 alveolar activity in infants with ARDS. PLoS One. 2012;7(10):e47066. doi: 10.1371/journal.pone.0047066. Epub 2012 Oct 11. PubMed PMID: 23071714; PubMed Central PMCID: PMC3469496.

4: 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.

5: De Luca D, Minucci A, Trias J, Tripodi D, Conti G, Zuppi C, Capoluongo E; Study Group on Secretory Phospholipase in Pediatrics. Varespladib inhibits secretory phospholipase A2 in bronchoalveolar lavage of different types of neonatal lung injury. J Clin Pharmacol. 2012 May;52(5):729-37. doi: 10.1177/0091270011405498. Epub 2011 May 20. PubMed PMID: 21602519.

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

7: 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.

8: 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.

9: 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.

10: 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.