Information Omarigliptin (MK-3102) 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). Targets DPP-4 (Cell-free assay) 1.6 nM 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 Glukagon under hyperglycaemic conditions. 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. 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 %.
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Omarigliptin (MK-3102)
Dangerous GoodsCAS number：1226781-44-7 molecular formula：C17H20F2N4O3S
overview
compound introduction
Specs
| Chinese alias | 奥格列汀 | 奥格列汀(MK-3102) | ||
| English alias | AC-28992 | J-690074 | MFCD22573261 | (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 | AKOS025289528 | CHEBI:134735 | (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6 | ||
| CAS number | 1226781-44-7 | molecular formula | C17H20F2N4O3S |
| molecular weight | 398.43 g/mol | Exact mass | - |
| PSA | 98.800 Ų | logp | 0.3 |
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physicochemical properties
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Safety information
pictogram：
GHS08 , GHS05 , GHS07
Signal word：
Danger
Hazard Statement：
H315: 引起皮肤刺激 H335: 可能引起呼吸道刺激 H341: 怀疑引起遗传缺陷 H413: 可能对水生生物造成长期的有害影响 H318: 造成严重的眼睛损伤 H317: 可能引起皮肤过敏反应 H334: 吸入可能引起过敏或哮喘病症状或呼吸困难 H370: 对器官造成损害 H361: 怀疑破坏生育力或未出生的孩子
Statement of Preventive Measures：
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P310: 立即致电解毒中心或医生。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P201:
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