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Omarigliptin (MK-3102) DPP inhibitor

Name: Omarigliptin (MK-3102)
Brand: Selleck Chemicals
SKU: S8565
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S8565

A competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM), Omarigliptin (MK-3102) 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).

Chemical Structure

Molecular Weight: 398.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.20

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Chemical Information, Storage & Stability

Molecular Weight	398.43	Formula	C₁₇H₂₀F₂N₄O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1226781-44-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CS(=O)(=O)N1C=C2CN(CC2=N1)C3CC(C(OC3)C4=C(C=CC(=C4)F)F)N

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (198.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.950mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 79 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.395mg/ml (0.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 7.9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	DPP-4 ^[1] (Cell-free assay) 1.6 nM
In vitro	Omarigliptin (MK-3102) is a potent inhibitor of DPP-4 and is highly selective over other proteases tested (IC50 > 67 μmol/L) with 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). It 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 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].
References	[1] https://pubmed.ncbi.nlm.nih.gov/24660890/ [2] https://pubmed.ncbi.nlm.nih.gov/26507988/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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