GRI 977143 |
| Catalog No.GC15865 |
An LPA2 receptor agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 325850-81-5
Sample solution is provided at 25 µL, 10mM.
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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).
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