Omarigliptin - CAS 1226781-44-7
Catalog number:
1226781-44-7
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
DPP4
Description:
Omarigliptin is a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor to be used as treatment for type 2 diabetes.
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Purity:
0.98
Appearance:
Solid powder
Synonyms:
MK3102; MK-3102; MK 3102; Omarigliptin
MSDS:
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1.Pharmacokinetic and Pharmacodynamic Effects of Multiple-dose Administration of Omarigliptin, a Once-weekly Dipeptidyl Peptidase-4 Inhibitor, in Obese Participants With and Without Type 2 Diabetes Mellitus.
Addy C1, Tatosian D2, Glasgow XS2, Gendrano IN 3rd2, Kauh E2, Martucci A2, Johnson-Levonas AO2, Selverian D2, Matthews CZ2, Gutierrez M3, Wagner JA2, Aubrey Stoch S2. Clin Ther. 2016 Mar;38(3):516-30. doi: 10.1016/j.clinthera.2015.12.020. Epub 2016 Feb 9.
PURPOSE: Omarigliptin (MK-3102) is a potent, oral, long-acting dipeptidyl peptidase (DPP)-4 inhibitor approved in Japan and in global development as a once-weekly treatment for type 2 diabetes mellitus (T2DM). The aim of this study was to investigate the pharmacokinetic (PK) and pharmacodynamic (PD) effects of omarigliptin in obese participants with and without T2DM.
2.Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.
Chen P1, Feng D1, Qian X1, Apgar J1, Wilkening R1, Kuethe JT1, Gao YD1, Scapin G1, Cox J1, Doss G2, Eiermann G3, He H2, Li X2, Lyons KA2, Metzger J4, Petrov A3, Wu JK4, Xu S2, Weber AE1, Yan Y1, Roy RS4, Biftu T1. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5767-71. doi: 10.1016/j.bmcl.2015.10.070. Epub 2015 Oct 30.
A series of novel substituted-[(3R)-amino-2-(2,5-difluorophenyl)]tetrahydro-2H-pyran analogs have been prepared and evaluated as potent, selective and orally active DPP-4 inhibitors. These efforts lead to the discovery of a long acting DPP-4 inhibitor, omarigliptin (MK-3102), which recently completed phase III clinical development and has been approved in Japan.
3.Safety and Efficacy of Omarigliptin (MK-3102), a Novel Once-Weekly DPP-4 Inhibitor for the Treatment of Patients With Type 2 Diabetes.
Sheu WH1, Gantz I2, Chen M3, Suryawanshi S3, Mirza A3, Goldstein BJ3, Kaufman KD3, Engel SS3. Diabetes Care. 2015 Nov;38(11):2106-14. doi: 10.2337/dc15-0109. Epub 2015 Aug 26.
OBJECTIVE: This study was conducted to determine the optimal dose of omarigliptin, a once-weekly (q.w.) dipeptidyl peptidase IV (DPP-4) inhibitor, for the treatment of patients with type 2 diabetes and evaluate the long-term safety of that dose.
4.Omarigliptin: first global approval.
Burness CB1. Drugs. 2015 Nov;75(16):1947-52. doi: 10.1007/s40265-015-0493-8.
Omarigliptin [Marizev(®) (Japan)] is a small-molecule dipeptidyl peptidase-4 (DPP-4) inhibitor developed by Merck for the oral treatment of type 2 diabetes (T2DM). Unlike the majority of other approved agents of its class, which are usually administered once daily, omarigliptin can be administered once weekly. Once-weekly omarigliptin has received its first global approval in this indication in Japan, for use in adults. Phase III clinical development of the product is underway in several other countries. This article summarizes the milestones in the development of omarigliptin leading to this first approval for the treatment of T2DM.
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CAS 1226781-44-7 Omarigliptin

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