Anagliptin

Anagliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4, IC50 = 3.8 nM). It is selective for DPP-4 over DPP-8 and DPP-9 (IC50s = 68 and 60 nM, respectively). Dietary administration of anagliptin (0.05 and 0.3% w/w) decreases plasma DPP-4 activity, increases plasma GLP-1 levels, suppresses food intake and body weight gain, ameliorates insulin resistance, and improves glucose tolerance in wild-type and glucokinase knockout mouse models of high-fat diet-induced diabetes. It decreases hepatic lipid and M1 macrophage accumulation and prevents hepatic fibrosis and steatohepatitis in mice fed a high-cholesterol high-fat diet or a choline-deficient L-amino acid-defined, high-fat (CDAHF) diet. Anagliptin also reduces atherosclerotic lesion size in an Apoe-/- mouse model of atherosclerosis.Formal Name: N-[2-[[2-[(2S)-2-cyano-1-pyrrolidinyl]-2-oxoethyl]amino]-2-methylpropyl]-2-methyl-pyrazolo[1,5-a]pyrimidine-6-carboxamide. CAS Number: 739366-20-2. Molecular Formula: C19H25N7O2. Formula Weight: 383.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml. lambdamax: 247 nm. SMILES: O=C(N1[C@@H](CCC1)C#N)CNC(C)(C)CNC(C2=CN3C(N=C2)=CC(C)=N3)=O. InChi Code: InChI=1S/C19H25N7O2/c1-13-7-16-21-9-14(11-26(16)24-13)18(28)22-12-19(2,3)23-10-17(27)25-6-4-5-15(25)8-20/h7,9,11,15,23H,4-6,10,12H2,1-3H3,(H,22,28)/t15-/m0/s1. InChi Key: LDXYBEHACFJIEL-HNNXBMFYSA-N.