GRI977143

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GRI977143 是特异性的 LPA2 受体的激动剂，其EC50 值为3.3 μM。

GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM .

GRI977143 (10 μM, 24-72 h) is effective in reducing activation of caspases 3, 7, 8, and 9 and inhibits poly(ADP-ribose)polymerase 1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis.GRI977143 is an effective stimulator of extracellular signal-regulated kinase 1/2 activation and promotes the assembly of a macromolecular signaling complex consisting of LPA2, Na+-H+ exchange regulatory factor 2, and thyroid receptor interacting protein 6.Cell Proliferation Assay Cell Line:Vector- and LPA2-transduced MEF cells (2 × 104).Concentration:10 μM.Incubation Time:24-72 h.Result:Did not cause a significant increase in vector cell proliferation except at 72 h (p < 0.05).Apoptosis Analysis.Cell Line:Doxorubicin-induced apoptotic signaling in vector-transduced or LPA2-transduced MEF.Concentration:10 μM.Incubation Time:24 h.Result:Reduced caspase 3 and 7 activation on LPA2-transduced MEF cells by 51 ± 3% and was approximately as potent as 3 μM LPA or OTP.Protected against doxorubicin-induced apoptosis by inhibiting caspase 3, 7, 8, and 9 and reducing DNA fragmentation.

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GPCR/G Protein

LPA Receptor

LPA Receptor

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325850-81-5

391.44

C22H17NO4S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (127.73 mM; 超声助溶 )

OC(=O)c1ccccc1SCCCN1C(=O)c2cccc3cccc(C1=O)c23

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(-20℃)

With Ice Pack

≥ 2 years