产品
编 号：F207543
分子式：C21H19N2NaO5
分子量：402.38
分子式：C21H19N2NaO5
分子量：402.38
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
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10mg
询价
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25mg
询价
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50mg
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结构图
CAS No: 172733-42-5
产品详情
生物活性：
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.
体内研究：
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.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.
体外研究：
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.
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.
体内研究：
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.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.
体外研究：
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.
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