sPLA2 9 nM (IC 50 )

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. Animal Model: Male Hartley guinea pigs (300-500 g) 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.

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. 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. Western Blot Analysis 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 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 (LY315920 sodium) 是一种有效且具有选择性的 group IIA, secretory phospholipase A2 (sPLA2) 抑制剂，其 IC50 值为 9 nM。Varespladib sodium 对大鼠，兔，豚鼠和人等各种物种血清的 sPLA2 活性具有明显的抑制作用，IC50 分别为 8.1 nM，5.0 nM，3.2 nM 和 6.2 nM。