Saxagliptin (hydrochloride) (Synonyms: BMS-477118) |
| カタログ番号GC44874 |
サクサグリプチン (塩酸塩) (BMS-477118 塩酸塩) は、強力、選択的、可逆的、競合的、経口的に活性なジペプチジルペプチダーゼ-4 (DPP-4) (Ki = 0.6-1.3 nM) 阻害剤です。
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Cas No.: 709031-78-7
Sample solution is provided at 25 µL, 10mM.
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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.
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