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4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

A synthetic small molecule that acts as a potent and selective inhibitor of dipeptidyl peptidase IV (DPP-4), an enzyme involved in the degradation of incretin hormones. This compound was developed as an experimental antidiabetic agent and considered a potential back-up candidate to sitagliptin for the treatment of type 2 diabetes mellitus. It demonstrated high potency (DPP-IV IC₅₀ = 2.6 nM), selectivity for DPP-IV over related enzymes, and efficacy in preclinical models such as oral glucose tolerance tests in mice[1][6][8]. The compound is not approved or marketed but has been studied extensively at the preclinical stage.

Other names
4-((3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl)-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)

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