CP 91,149

CP 91,149 is an inhibitor of human liver glycogen phosphorylase a (LGPa), muscle glycogen phosphorylase a (MGPa), and MGPb (IC50s = 0.13, 0.2, and 0.3 µM, respectively, in the presence of glucose). CP 91,149 is 5- to 10-fold less potent in the absence of glucose. In vitro, it inhibits glucagon-stimulated glycogenolysis in primary human hepatocytes (IC50 = 2.1 µM) and increases glycogen synthesis in rat hepatocytes at a concentration of 2.5 µM in the presence of 5 mM glucose. CP 91,149 inhibits brain GP (IC50 = 0.5 µM) and, at a concentration of 30 µM, inhibits glycogen accumulation and proliferation of A549 non-small cell lung carcinoma (NSCLC) cells that express endogenous brain GP. In vivo, CP 91,149 (25 mg/kg, p.o.) lowers the plasma glucose level in diabetic ob/ob mice within 3 hours of administration without producing hypoglycemia, but has no effect on normoglycemic, non-diabetic mice.Formal Name: 5-chloro-N-[(1S,2R)-3-(dimethylamino)-2-hydroxy-3-oxo-1-(phenylmethyl)propyl]-1H-indole-2-carboxamide. CAS Number: 186392-40-5. Molecular Formula: C21H22ClN3O3. Formula Weight: 399.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml. lambdamax: 212, 298 nm. SMILES: ClC1=CC=C2C(C=C(C(N[C@@]([C@@H](O)C(N(C)C)=O)([H])CC3=CC=CC=C3)=O)N2)=C1. InChi Code: InChI=1S/C21H22ClN3O3/c1-25(2)21(28)19(26)17(10-13-6-4-3-5-7-13)24-20(27)18-12-14-11-15(22)8-9-16(14)23-18/h3-9,11-12,17,19,23,26H,10H2,1-2H3,(H,24,27)/t17-,19+/m0/s1. InChi Key: HINJNZFCMLSBCI-PKOBYXMFSA-N.