[CAS NO. 1226781-44-7] Omarigliptin (MK-3102)

Name: Omarigliptin (MK-3102)
Brand: Arctom Scientific
SKU: SLK-S8565

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PRODUCTS SPECIFICATIONS [1226781-44-7]

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Catalog

SLK-S8565

Brand

Selleck

CAS

1226781-44-7

DESCRIPTION [1226781-44-7]

Overview

MDL	MFCD22573261
Molecular Weight	398.43
Molecular Formula	C17H20F2N4O3S
SMILES	S(C)(=O)(=O)N1C=C2C(CN(C2)[C@@]3(C[C@H](N)[C@](OC3)(C4=C(F)C=CC(F)=C4)[H])[H])=N1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.5099 mL	12.5493 mL	25.0985 mL
5 mM	0.5020 mL	2.5099 mL	5.0197 mL
10 mM	0.2510 mL	1.2549 mL	2.5099 mL
50 mM	0.0502 mL	0.2510 mL	0.5020 mL

Description

Omarigliptin (MK-3102) is a competitive, reversible inhibitor of (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

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.

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. 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 %.

References

[1] Biftu T, et al. J Med Chem. 2014, 57(8):3205-12.
[2] Burness CB, et al. Drugs. 2015, 75(16):1947-52.

Synonyms

2H-Pyran-3-amine, 2-(2,5-difluorophenyl)-5-[2,6-dihydro-2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-, (2R,3S,5R)-

(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2,6-dihydro-2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine

(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine

Omarigliptin