(-)-Sitagliptin carbamoyl glucuronide is a minor phase II metabolite of the dipeptidylpeptidase 4 (DPP-4) inhibitor (-)-sitagliptin . (-)-Sitagliptin carbamoyl glucuronide is formed by N-carbamoyl glucuronidation and has been found in rat and dog plasma following administration of (-)-sitagliptin.
Sitagliptin N-sulfate is a phase II metabolite of the dipeptidylpeptidase 4 (DPP-4) inhibitor (-)-sitagliptin . Sitagliptin N-sulfate is formed via sulfation and has been found in rat bile following oral administration of (-)-sitagliptin.
Melogliptin, also known as EMD-675992 and GRC-8200, is a potent and selective a dipeptidylpeptidase IV (DPP-IV) inhibitor potentially for treatment of type II diabetes. Melogliptin significantly reduced HbA1c from baseline as compared to placebo with a mean average reduction of 0.75 percent in patients receiving 50mg twice daily dose and 0.60 percent in patients receiving 100 mg once daily dose.
DPP IV hCA II-IN-1 是一种有效的选择性二肽肽酶 IV (DPP IV) 和碳酸酐酶 (CA) 抑制剂,抑制 DPP IV 的 IC50值为 0.049 μM, 抑制 CA II、CA VB、CA VA、CA IX、CA I 和 CA IV 的 Ki 值分别为 0.0361、0.0428、0.0941、0.1328、0.2615 和 3.034 μM。