A neuropeptide with diverse biological activities
货号:ajcx23458
CAS:N/A
分子式:C17[13C]H23D2N3O2.HCl
分子量：354.9
溶解度:DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 2 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Saxagliptin-¹³C-d₂is intended for use as an internal standard for the quantification of saxagliptin by GC- or LC-MS. Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; K_i= 0.6 nM).¹It inhibits DPP-4ex vivo(ED₅₀= 0.12 μmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zucker^fa/fadiabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 μmol/kg increases plasma insulin levels and improves glucose clearance inob/obmice, 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.²Formulations containing saxagliptin have been used for the treatment of type 2 diabetes.

1.Augeri, D.J., Robl, J.A., Betebenner, D.A., et al.Discovery and preclinical profile of Saxagliptin (BMS-477118): A highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetesJ. Med. Chem.48(15)5025-5037(2005) 2.Koyani, C.N., Kolesnik, E., WÖlkart, G., et al.Dipeptidyl peptidase-4 independent cardiac dysfunction links saxagliptin to heart failureBiochem. Pharmacol.145(1)64-80(2017)