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GRI 977143
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。
GRI 977143图片
CAS NO:325850-81-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
GRI 977143 是一种特异性 LPA2 受体激动剂,EC50 为 3.3 μM。
Cas No.325850-81-5
化学名2-[3-(1,3-dioxobenzo[de]isoquinolin-2-yl)propylsulfanyl]benzoic acid
Canonical SMILESC1=CC=C(C(=C1)C(=O)O)SCCCN2C(=O)C3=CC=CC4=C3C(=CC=C4)C2=O
分子式C22H17NO4S
分子量391.44
溶解度10mg/mL in DMSO,10mg/mL in DMF
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GRI-977143 is an agonist of G protein-coupled lysophosphatidic acid receptor 2 (LPA2) with an EC50 value of 3.3 μM in LPA2-transfected RH7777 cells.[1] It is selective for LPA2, having no activity at LPA1, LPA3, LPA4, and LPA5 at concentrations up to 10 μM. GRI-977143 increases growth and reduces caspase-3 and -7 activation in LPA2-transduced MEF fibroblasts. It increases MM1 rat hepatoma cell invasion and inhibits apoptosis of IEC-6 cells induced by TNF-α, doxorubicin, or serum withdrawal. GRI-977143 also rescues apoptotic cells from γ-irradiation-induced injury in vitro and in vivo.[2]

Reference:
[1]. Kiss, G.N., Fells, J.I., Gupte, R.D., et al. Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions. Mol. Pharmacol. 82(6), 1162-1173 (2012).
[2]. Kiss, G.N., Lee, S.-C., Fells, J., et al. Mitigation of radiation injury by selective stimulation of the LPA2 receptor. Biochim. Biophys. Acta 1831(1), 117-125 (2013).