Omarigliptin

Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over allproteases tested (IC50 > 67 μM).IC50 value: 1.6 nM [1]Target: DPP-4 inhibitorin vitro: Omarigliptin has weak ion channel activity (IC50 > 30 μM at IKr, Cav1.2, and Nav1.5). An expansive selectivity counterscreen (168 radioligand binding or enzymatic assays) was carried out at MDS Pharma. An IC50 > 10 μM was obtained in all assays. in vivo: When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test (OGTT), it significantly reduced blood glucose excursion in a dose-dependent manner from 0.01 mg/kg (7% reduction in glucose AUC) to 0.3 mg/kg (51% reduction).

Signaling Pathways >> Metabolic Enzyme/Protease >> Dipeptidyl Peptidase

Research Areas >> Metabolic Disease

[1]. Biftu T, et al. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014 Apr 24;57(8):3205-12.

Talabostat mesylate | Linagliptin | Teneligliptin | Vildagliptin (LAF-237) | AZD7986 | Anagliptin | Trelagliptin | Gemigliptin | DPP-IV-IN-2 | DBPR108 | Diprotin A TFA (Ile-Pro-Pro (TFA)) | Saikogenin A | UAMC 00039 dihydrochloride | Dutogliptin | Gosogliptin