Saxagliptin (hydrochloride)

Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4, Ki = 0.6 nM). It inhibits DPP-4 ex vivo (ED50 = 0.12 µmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zuckerfa/fa diabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 µmol/kg increases plasma insulin levels and improves glucose clearance in ob/ob mice, a transgenic model of obesity. Saxagliptin induces systolic and diastolic dysfunction, reduces contractile force, and exacerbates ischemia-reperfusion injury-induced cardiac dysfunction in isolated guinea pig hearts. Formulations containing saxagliptin have been used for the treatment of type 2 diabetes.Formal Name: (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile, monohydrochloride. CAS Number: 709031-78-7. Synonyms: BMS-477118. Molecular Formula: C18H25N3O2 . HCl. Formula Weight: 351.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 10 mg/ml, PBS (pH 7.2): 2 mg/ml. lambdamax: 202 nm. SMILES: O=C(N1[C@H](C#N)C[C@H]2[C@@H]1C2)[C@H]([C@@]3(C[C@H](C4)C5)C[C@H]5C[C@@]4(O)C3)N.Cl. InChi Code: InChI=1S/C18H25N3O2.ClH/c19-8-13-2-12-3-14(12)21(13)16(22)15(20)17-4-10-1-11(5-17)7-18(23,6-10)9-17,/h10-15,23H,1-7,9,20H2,1H/t10-,11+,12-,13?,14+,15-,17+,18-,/m1./s1. InChi Key: TUAZNHHHYVBVBR-WYHYZCDFSA-N.