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Omarigliptin

Names

[ CAS No. ]:
1226781-44-7

[ Name ]:
Omarigliptin

[Synonym ]:
UNII-CVP59Q4JE1
(2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]-tetrahydro-2H-pyran-3-amine
MK-3102
Omarigliptin
(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine
2H-Pyran-3-amine, 2-(2,5-difluorophenyl)-5-[2,6-dihydro-2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-, (2R,3S,5R)-
MK-3102

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Dipeptidyl Peptidase
Research Areas >> Metabolic Disease

[References]

[1]. Biftu T, et al. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014 Apr 24;57(8):3205-12.


[Related Small Molecules]

Talabostat mesylate | Linagliptin | Teneligliptin | Vildagliptin (LAF-237) | AZD7986 | Anagliptin | Trelagliptin | Gemigliptin | DPP-IV-IN-2 | DBPR108 | Diprotin A TFA (Ile-Pro-Pro (TFA)) | Saikogenin A | UAMC 00039 dihydrochloride | Dutogliptin | Gosogliptin

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
529.4±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C17H20F2N4O3S

[ Molecular Weight ]:
398.427

[ Flash Point ]:
274.0±32.9 °C

[ Exact Mass ]:
398.122406

[ PSA ]:
98.83000

[ LogP ]:
0.46

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.689

[ Storage condition ]:
-20℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds