1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Omarigliptin

Omarigliptin (Synonyms: MK-3102)

Cat. No.: HY-15981
Handling Instructions

Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all proteases tested (IC50 > 67 μM).

For research use only. We do not sell to patients.

Omarigliptin Chemical Structure

Omarigliptin Chemical Structure

CAS No. : 1226781-44-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 168 In-stock
Estimated Time of Arrival: December 31
2 mg USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 650 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all proteases tested (IC50 > 67 μM). IC50 value: 1.6 nM [1] Target: DPP-4 inhibitor in 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).

Clinical Trial
Molecular Weight

398.43

Formula

C₁₇H₂₀F₂N₄O₃S

CAS No.
SMILES

N[[email protected]@H]1[[email protected]@H](C2=CC(F)=CC=C2F)OC[[email protected]](N3CC4=NN(S(=O)(C)=O)C=C4C3)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (125.49 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

OmarigliptinMK-3102MK3102MK 3102Dipeptidyl PeptidaseDPPInhibitorinhibitorinhibit

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Omarigliptin
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HY-15981
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