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Varespladib sodium

产品编号 T39173 CAS 172733-42-5

别名: LY315920 sodium, 伐瑞拉迪钠；伐瑞拉地钠

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.

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Varespladib sodium, CAS 172733-42-5

规格	价格/CNY	货期
2 mg	￥ 822	5日内发货
5 mg	￥ 1,370	5日内发货
10 mg	￥ 2,190	5日内发货

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Varespladib sodium 的其他形式现货产品:

Varespladib

其他形式的 Varespladib sodium:

Varespladib
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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	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.
靶点活性	SPLA2:9 nM (IC50)
体外活性	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.
体内活性	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.

别名	LY315920 sodium, 伐瑞拉迪钠；伐瑞拉地钠
分子量	403.39
分子式	C21H20N2NaO5
CAS No.	172733-42-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

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. 1999 Mar;288(3):1117-24. 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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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