R-59-949

R-59-949 is an inhibitor of diacylglycerol kinase alpha (DGK-alpha) with an IC50 value of 300 nM in isolated platelet plasma membranes using exogenous diacylglycerol as a substrate. DGK-alpha inhibition with R-59-949 increases diacylglycerol-dependent PKC activity, serotonin secretion, and aggregation of thrombin-stimulated platelets. R-59-949 inhibits DGK-alpha activity induced by platelet-derived growth factor (PDGF) in intact vascular smooth muscle cells (VSMCs). It inhibits high K+- and glucose-induced insulin secretion in MIN6 pancreatic beta-cells in a dose-dependent manner. In vivo, administration of R-59-949 prevents retinal neovascularization in a mouse model of oxygen-induced retinopathy.Formal Name: 3-[2-[4-[bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone. CAS Number: 120166-69-0. Synonyms: Diacylglycerol Kinase Inhibitor II, DKGI-II. Molecular Formula: C28H25F2N3OS. Formula Weight: 489.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMSO: 33 mg/ml, Ethanol: 1 mg/ml. lambdamax: 294 nm. SMILES: S=C1N(CCN2CC/C(CC2)=C(C3=CC=C(F)C=C3)/C4=CC=C(F)C=C4)C(C5=CC=CC=C5N1)=O. InChi Code: InChI=1S/C28H25F2N3OS/c29-22-9-5-19(6-10-22)26(20-7-11-23(30)12-8-20)21-13-15-32(16-14-21)17-18-33-27(34)24-3-1-2-4-25(24)31-28(33)35/h1-12H,13-18H2,(H,31,35). InChi Key: ZCNBZFRECRPCKU-UHFFFAOYSA-N.