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Varespladib

Chemical Structure : Varespladib

CAS No.: 172732-68-2

Varespladib (LY 315920;LY315920;LY-315920;A-002)

Catalog No.: PC-43510Not For Human Use, Lab Use Only.

Varespladib (LY315920, A-002) is a potent, selective inhibitor of recombinant human, group IIA, nonpancreatic secretory PLA2 (sPLA2) with IC50 of 9 nM, 40-fold less active against group IB, pancreatic sPLA2 and inactive against cytosolic PLA2.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Varespladib (LY315920, A-002) is a potent, selective inhibitor of recombinant human, group IIA, nonpancreatic secretory PLA2 (sPLA2) with IC50 of 9 nM, 40-fold less active against group IB, pancreatic sPLA2 and inactive against cytosolic PLA2.
Varespladib (LY315920, A-002) inhibits human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells with IC50 of 0.79 uM.
Varespladib (LY315920, A-002) suppresses sPLA2 produced contractile responses in guinea pig lung pleural strips with KB of 83 nM.
Varespladib (LY315920, A-002) reduces atherosclerosis and aneurysm formation in ApoE-/- mice.

Physicochemical Properties

M.Wt 380.39
Formula C21H20N2O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

Acetic acid, 2-[[3-(2-amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]-

References

1. Snyder DW, et al. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.

2. Draheim SE, et al. J Med Chem. 1996 Dec 20;39(26):5159-75.

3. Fraser H, et al. J Cardiovasc Pharmacol. 2009 Jan;53(1):60-5.

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