Varespladib sodium_product_DataBase

Bioactivity	Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively[1].
Invitro	Varespladib sodium (10 μM; 24 and 48 hours; HCjE cells) treatment results in complete inhibition of the RA-induced increase in MUC16 protein detected in cell lysates at both time points[2].Varespladib sodium (10 μM; 24 and 48 hours; HCjE cells) treatment significantly inhibits RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours[2]. Western Blot Analysis[2] Cell Line:
In Vivo	Varespladib sodium treatment inhibits human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells with an IC50 of 0.79 μM. And the ED50 for Varespladib sodium is 16.1 mg/kg[1]. Animal Model:
Name	Varespladib sodium
CAS	172733-42-5
Formula	C21H19N2NaO5
Molar Mass	402.38
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Snyder DW, et al. Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. J Pharmacol Exp Ther. 1 [2]. Hori Y, et al. Effect of retinoic acid on gene expression in human conjunctival epithelium: secretory phospholipase A2 mediates retinoic acid induction of MUC16. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4050-61.

PeptideDB

Varespladib sodium

CAS: 172733-42-5 F: C21H19N2NaO5 W: 402.38