LY-315920
- CAS号:172733-42-5
- 英文名:NATRIUM[(1-BENZYL-2-ETHYL-3-OXAMOYLINDOOL-4-YL)OXY]ACETAAT
- 中文名:LY-315920
- CBNumber:CB01475683
- 分子式:C21H21N2NaO5
- 分子量:404.4
- MOL File:172733-42-5.mol
- 形态 :Solid
- 颜色 :Off-white to light yellow
LY-315920性质、用途与生产工艺
- 生物活性 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。
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靶点
sPLA2
9 nM (IC 50 )
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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.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. -
体内研究
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.
- 更新日期：2024/11/08
- 产品编号：HY-13402A
- 产品名称：Varespladib sodium
- CAS编号：
- 包装：1 mg
- 价格：750元
- 更新日期：2024/11/08
- 产品编号：HY-13402A
- 产品名称：Varespladib sodium
- CAS编号：
- 包装：5 mg
- 价格：1650元
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
