Varespladib Sodium

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Varespladib Sodium

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

172733-42-5

LY315920 sodium

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。

生物活性

Varespladib sodium (LY315920 sodium) is a potent and selectivegroup IIA, secretoryphospholipase A₂(sPLA₂)inhibitor with anIC₅₀of 9 nM. Varespladib sodium exhibits the significant inhibitory effect onsPLA2activity in serum from various species including rat, rabbit, guinea pig and human withIC₅₀s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively^[1].

IC₅₀& Target

sPLA2

9 nM (IC₅₀)

体外研究
(In Vitro)

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.

体内研究
(In Vivo)

Varespladib sodium treatment inhibits human sPLA₂-induced release of thromboxane A₂(TXA₂) from isolated guinea pig lung bronchoalveolar lavage cells with anIC₅₀of 0.79 μM. And theED₅₀for 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.

Clinical Trial

分子量

402.38

Formula

C₂₁H₁₉N₂NaO₅

CAS 号

172733-42-5

中文名称

伐瑞拉迪钠；伐瑞拉地钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.