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Fig. 1 · Structure
Cat. No.
A13310
CAS No.
1226781-44-7
Formula
C17H20F2N4O3S
Mol. Weight
398.43

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MK-3102

Cat. No. A13310 CAS 1226781-44-7

DPP-4 inhibitor

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).

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
COS-7 IC50 > 100000 nM Inhibition of C-terminal His-tagged DPP8 (unknown origin) expressed in COS7 cells using H-Ala-Pro-pNA substrate preincubated for 15 mins [PMID: 26546218]
Sf9 IC50 > 100000 nM Inhibition of N-terminal FLAG tagged human QPP expressed in Sf9 cells using Nle-Pro-AMC substrate after 30 mins by plate reader analysis [PMID: 26546218]
Sf9 IC50 2.22 nM Inhibition of DPP4 (unknown origin) expressed in Sf9 cells using Gly-Pro-AMC substrate [PMID: 27396490]
Sf9 IC50 2.6 nM Inhibition of recombinant human DPP4 expressed in Sf9 cells using Gly-Pro-AMC substrate after 30 mins by plate reader analysis [PMID: 26546218]

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1226781-44-7
Applications DPP-4 inhibitor
Formula C17H20F2N4O3S
Molecular Weight 398.43
SMILES
CS(=O)(=O)N1C=C2CN(CC2=N1)[C@@H]3C[C@@H]([C@H](OC3)C4=C(C=CC(=C4)F)F)N

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 77 mg/mL (193.25 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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