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Technical Data
| Formula | C17H20F2N4O3S |
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| Molecular Weight | 398.43 | CAS No. | 1226781-44-7 | |
| Solubility (25°C)* | In vitro | DMSO | 79 mg/mL (198.27 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
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). | ||
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| Targets |
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| 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 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]. |
Protocol (from reference)
References
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Selleck's Omarigliptin (MK-3102) has been cited by 2 publications
| Distal mutation V486M disrupts the catalytic activity of DPP4 by affecting the flap of the propeller domain [ Acta Pharmacol Sin, 2021, 1-9] | PubMed: 34907358 |
| Intranasal Neuropeptide Y as a Potential Therapeutic for Depressive Behavior in the Rodent Single Prolonged Stress Model in Females [ Front Behav Neurosci, 2021, 15:705579] | PubMed: 34566592 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.