Home Proteases DPP inhibitor Omarigliptin (MK-3102) For research use only.

Omarigliptin (MK-3102)

Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5).

Omarigliptin (MK-3102) Chemical Structure

Omarigliptin (MK-3102) Chemical Structure

CAS No. 1226781-44-7

Purity & Quality Control

Batch: S856501 DMSO]79 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.20%
99.20

Omarigliptin (MK-3102) Related Products

Signaling Pathway

DPP Signaling Pathways

DPP Signaling Pathway

Biological Activity

Description Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5).
Targets
DPP-4 [1]
(Cell-free assay)
1.6 nM
In vitro
In vitro Omarigliptin is a potent inhibitor of DPP-4 and is highly selective over other proteases tested (IC50 > 67 μmol/L) and has weak ion channel activity (IC50 > 30 μmol/L at IKr, Caγ1.2, and Naγ1.5). Additionally, an IC50 > 10 μmol/L was obtained in all assays in an expansive selectivity counterscreen (168 radioligand binding or enzymatic assays). Omarigliptin binds rapidly and competitively to the active site of DPP-4, a process that is reversible and highly selective, and thus leads to increased levels of insulin and decreased levels of glucagon under hyperglycaemic conditions[2].
In Vivo
In vivo In lean mice, 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). the administration of omarigliptin dose-dependently increases plasma concentrations of active GLP-1. The pharmacokinetics of omarigliptin in male Sprague−Dawley rat and beagle dog are characterized by a low plasma clearance (0.9−1.1 mL/min/kg), a volume of distribution at steady state of 0.8−1.3 L/kg, and a long terminal half-life (∼11−22 h). The oral bioavailability of omarigliptin is good in both dogs and rats (∼100%). Omarigliptin is well-tolerated over the duration of the study, with no mortality or physical signs noted[1]. Following the administration of a single oral dose of 25 mg in volunteers, omarigliptin was rapidly absorbed, with peak concentrations (Cmax) of 750 nmol/L reached within 1 h (Tmax). Bioavailability was estimated to be ≥74 %[2].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02906709 Completed
Type 2 Diabetes Mellitus
Merck Sharp & Dohme LLC
 October 17 2016 Phase 4
NCT01407276 Completed
Chronic Renal Insufficiency|Type 2 Diabetes Mellitus
Merck Sharp & Dohme LLC
 August 8 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 398.43 Formula

C17H20F2N4O3S
CAS No. 1226781-44-7 SDF Download Omarigliptin (MK-3102) SDF
Smiles CS(=O)(=O)N1C=C2CN(CC2=N1)C3CC(C(OC3)C4=C(C=CC(=C4)F)F)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (198.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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