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CAS No.: 1226781-44-7

奥格列汀 Catalog No. CSN13845

Synonyms: MK-3102

Omarigliptin, also called MA-3102, is an selective inhibitor of DPP-4 with IC50 of 1.6 nM and Ki of 0.8 nM. Its selectivity is higher than other 168 proteasomes.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 DPP4

IC50:1.6nM
描述Omarigliptin is a competitive, potent and selective inhibitor of dipeptidyl peptidase 4 (DPP-4) (IC50 = 1.6 nM, Ki = 0.8 nM) developed for the treatment of type 2 diabetes, which is highly selective over all proteases tested (IC50 > 67 μM). Omarigliptin has weak ion channel activity (IC50 > 30 μM at IKr, Cav1.2, and Nav1.5)^[3]. Omarigliptin is indicated to have favorable effects on glycosylated hemoglobin (HbA1c), fasting and postmeal plasma glucose^[4]. Omarigliptin improves glucose control in patients with type 2 diabetes by increasing the circulating concentration of glucagon-like peptide 1 and glucose-dependent insulinotropic polypeptide. Administration of omarigliptin dose-dependently increased plasma concentrations of active GLP-1, with maximal increases in active GLP-1 observed at the 0.3 to 1 mg/kg doses^[3]. Omarigliptin resulted in ∼2-fold increases in weighted average postprandial active GLP-1. The average renal clearance of omarigliptin was ∼2 L/h and DPP-4 inhibition ranged from ∼77% to 89% at 168 hours ^[5].When orally administered 1 h prior to dextrose challenge, omarigliptin 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 lean mice^[3]. The oral bioavailability of omarigliptin was good in both dogs and rats (∼100%),and the mean percentage of unbound omarigliptin (1, 10, and 100 μM) in CD-1 mouse, Sprague–Dawley rat, beagle dog, and human plasma was 38%, 15%, 43%, and 68%, respectively^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01217073	Type 2 Diabetes Mellitus	Phase 2	Completed	-	-
NCT01682759	Type 2 Diabetes Mellitus	Phase 3	Completed	-	-
NCT01841697	Type 2 Diabetes	Phase 3	Completed	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5099 mL
- 12.5493 mL
- 25.0987 mL
- 5 mM
- 0.5020 mL
- 2.5099 mL
- 5.0197 mL
- 10 mM
- 0.2510 mL
- 1.2549 mL
- 2.5099 mL

技术信息

CAS号

1226781-44-7

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H20F2N4O3S

运输

蓝冰

分子量

398.43

别名

MK-3102

溶解度

DMSO	78.0 mg/mL (195.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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