Omarigliptin chemical structure
Chemical structureResearch use only
CAT. NO. DC7585Featured

Omarigliptin

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Product overview

Description & Application

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).

ParameterValue
Chemical NameOmarigliptin
CAS No.1226781-44-7
SynonymsMK－3012;(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine;(2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)oxan-3-amine;(2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3...;MK-3102;Omarigliptin;Omarigliptin (MK3102);(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;MK3102;UNII-CVP59Q4JE1;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;(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;Omarigliptin [USAN:INN];AK170357;Tube;OMARIGLIPTIN;OMARIGLIPTIN;MK-3102Omarigliptin?;MK-3102Omarigliptin?;CHEBI:134735;CHEBI:134735;OMARIGLIPTIN [WHO-DD];OMARIGLIPTIN [WHO-DD];AKOS025289528;AKOS025289528;MKMPWKUAHLTIBJ-ISTRZQFTSA-N;MKMPWKUAHLTIBJ-ISTRZQFTSA-N;NSC-802900;NSC-802900;NSC802900;NSC802900;AC-28992;AC-28992;OMARIGLIPTIN [INN];OMARIGLIPTIN [INN];CHEMBL2105762;CHEMBL2105762;(2R,3S,5R)-2-(2,5-DIFLUOROPHENYL)-5-(2-(METHYLSULFONYL)PYRROLO[3,4-C]PYRAZOL-5(2H,4H,6H)-YL)TETRAHYDRO-2H-PYRAN-3-AMINE;(2R,3S,5R)-2-(2,5-DIFLUOROPHENYL)-5-(2-(METHYLSULFONYL)PYRROLO[3,4-C]PYRAZOL-5(2H,4H,6H)-YL)TETRAHYDRO-2H-PYRAN-3-AMINE;J-690074;J-690074;HY-15981;HY-15981;NS00073001;NS00073001;(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-(2-(methanesulfonyl)-2,6-dihydropyrrolo(3,4- c)pyrazol-5(4H)-yl)oxan-3-amine;(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-(2-(methanesulfonyl)-2,6-dihydropyrrolo(3,4- c)pyrazol-5(4H)-yl)oxan-3-amine;OMARIGLIPTIN [MI];OMARIGLIPTIN [MI];Omarigliptin (JAN/USAN/INN);Omarigliptin (JAN/USAN/INN);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)-;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)-;s8565;s8565;BDBM50003020;SCHEMBL827590;BDBM50003020;1226781-44-7;SCHEMBL827590;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)-;1226781-44-7;Omarigliptin (MK-3102);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)-;EX-A395;Omarigliptin (MK-3102);D10317;EX-A395;GTPL8402;D10317;AM85511;GTPL8402;DTXSID70153678;AM85511;DS-7574;DTXSID70153678;CCG-268634;DS-7574;MFCD22573261;CCG-268634;OMARIGLIPTIN [JAN];MFCD22573261;PB39113;OMARIGLIPTIN [JAN];(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;PB39113;NCGC00480770-01;Q21098979;(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-(2-(m...
FormulaC17H20F2N4O3S
M.Wt398.4275
SMILESS(C([H])([H])[H])(N1C([H])=C2C(C([H])([H])N(C2([H])[H])[C@@]2([H])C([H])([H])O[C@]([H])(C3C([H])=C(C([H])=C([H])C=3F)F)[C@]([H])(C2([H])[H])N([H])[H])=N1)(=O)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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).

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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