GRI977143

Research use only, not for human use.

GRI977143 is a selective and non-lipid agonist of LPA2 (EC50 = 3.3 μM). GRI977143 inhibits the activation of caspases 3, 7, 8, and 9 and and reduces DNA fragmentation.

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.

——

——

GPCR/G Protein

LPA Receptor

LPA Receptor

——

——

325850-81-5

391.44

C22H17NO4S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (127.73 mM; Ultrasonic )

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

——

(-20℃)

With Ice Pack

≥ 2 years