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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-GRI 977143
GRI 977143

Chemical Structure : GRI 977143

CAS No.: 325850-81-5

GRI 977143 (GRI977143;GRI-977143)

货号: PC-60890Not For Human Use, Lab Use Only.

A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).

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10 mg ¥1980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GRI 977143 is a potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).
GRI 977143 also inhibits LPA3 with IC50 of 6.6 uM.
GRI 977143 reduces the activation of caspases 3, 7, 8 and 9 and inhibits PARP1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis in vitro.
GRI 977143 promotes carcinoma cell invasion of human umbilical vein endothelial cell monolayers and fibroblast proliferation.

物理化学性质&存储条件

分子量 391.44
分子式 C22H17NO4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic acid

参考文献

1. Kiss GN, et al. Mol Pharmacol. 2012 Dec;82(6):1162-73.

2. Lin KH, et al. Sci Rep. 2016 May 31;6:27050.

3. Patil R, et al. Chem Biol. 2015 Feb 19;22(2):206-16.

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