MK-0557

MK-0557 is a potent antagonist of the neuropeptide Y (NPY) receptor Y5 (Kis = 1.3, 0.79, 0.74, and 1.4 nM for human, rhesus monkey, mouse, and rat receptors, respectively). It is >7,500-fold selective for Y5 over other receptors and lacks activity in a panel of 180 receptors, enzymes, and ion channels at concentrations up to 1 µM. MK-0557 increases intracellular calcium in CHO cells expressing the human Y5 receptor in a concentration-dependent manner. In vivo, MK-0557 (30 mg/kg) reduces body weight gain in wild-type and diet-induced obese mice. It also reduces retroperitoneal fat pad weight, epididymal and mesenteric fat pad weights, leptin levels, and food intake in lean mice fed a high-fat diet.Formal Name: trans-N-[1-(2-fluorophenyl)-1H-pyrazol-3-yl]-1'-oxo-spiro[cyclohexane-1,3'(1'H)-furo[3,4-c]pyridine]-4-carboxamide. CAS Number: 328232-95-7. Molecular Formula: C22H19FN4O3. Formula Weight: 406.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 3 mg/ml. lambdamax: 271 nm. SMILES: O=C(O1)C2=C(C=NC=C2)[C@]31CC[C@H](C(NC4=NN(C5=CC=CC=C5F)C=C4)=O)CC3. InChi Code: InChI=1S/C22H19FN4O3/c23-17-3-1-2-4-18(17)27-12-8-19(26-27)25-20(28)14-5-9-22(10-6-14)16-13-24-11-7-15(16)21(29)30-22/h1-4,7-8,11-14H,5-6,9-10H2,(H,25,26,28)/t14-,22-. InChi Key: RMYZIRFUCOMQRH-CAJLXGCNSA-N.