Varespladib sodium (LY315920 sodium) is a highly potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), with an IC50 of 9 nM. It demonstrates significant inhibitory activity against sPLA2 in serum samples from multiple species, including rat, rabbit, guinea pig, and human, with IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively.

SPLA2:9 nM (IC50)

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: HCjE cells Concentration: 10 μM Incubation Time: 24 hours, 48 hours Result: Significantly inhibited the RA-induced MUC16 protein expression at both time points. RT-PCR[2]Cell Line: HCjE cells Concentration: 10 μM Incubation Time: 24 hours, 48 hours Result: Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.

Varespladib sodium treatment inhibits human sPLA 2 -induced release of thromboxane A 2 (TXA 2 ) from isolated guinea pig lung bronchoalveolar lavage cells with an IC 50 of 0.79 μM. And the ED 50 for Varespladib sodium is 16.1 mg/kg[1]. Animal Model: Male Hartley guinea pigs (300-500 g)[1]Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg Administration: Intravenous injection (Pharmacokinetic study) Result: Consistent inhibition of sPLA2 activity in BAL fluid was observed. Reduced the human sPLA2-induced generation of TXA2 on BAL cells from guinea pigs.