GRI-977143

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. 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-alpha, doxorubicin (Cay-15007), or serum withdrawal. GRI-977143 also rescues apoptotic cells from gamma-irradiation-induced injury in vitro and in vivo.Formal Name: 2-[[3-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]-benzoic acid. CAS Number: 325850-81-5. Molecular Formula: C22H17NO4S. Formula Weight: 391.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:40): 0.025 mg/ml. lambdamax: 232 nm. SMILES: O=C(O)C1=CC=CC=C1SCCCN2C(C3=C4C(C2=O)=CC=CC4=CC=C3)=O. InChi Code: InChI=1S/C22H17NO4S/c24-20-16-9-3-6-14-7-4-10-17(19(14)16)21(25)23(20)12-5-13-28-18-11-2-1-8-15(18)22(26)27/h1-4,6-11H,5,12-13H2,(H,26,27). InChi Key: GMVZUCHUOYUMLL-UHFFFAOYSA-N.