SB-408124

SB-408124 is a potent antagonist of orexin 1 receptors (OX1Rs) with a Ki value of 26.9 nM in a calcium mobilization assay using CHO cells that stably express human OX1R. It is selective for OX1R over OX2R, with Kd values of 21.7 and 1,704 nM, respectively, in a radioligand binding assay. In vivo co-perfusion of SB-408124 with human OX1R in the rat ventral tegmental area inhibits OX1R-induced glutamate and dopamine elevations and reduces cocaine-seeking behavior in rats.Formal Name: N-(6,8-difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]-urea. CAS Number: 288150-92-5. Molecular Formula: C19H18F2N4O. Formula Weight: 356.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 20 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 227, 265, 315 nm. SMILES: FC1=CC(F)=CC2=C1N=C(C)C=C2NC(NC3=CC=C(N(C)C)C=C3)=O. InChi Code: InChI=1S/C19H18F2N4O/c1-11-8-17(15-9-12(20)10-16(21)18(15)22-11)24-19(26)23-13-4-6-14(7-5-13)25(2)3/h4-10H,1-3H3,(H2,22,23,24,26). InChi Key: JTARFZSNUAGHRB-UHFFFAOYSA-N.