Omarigliptin B

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Omarigliptin (MK-3102) 是一种有效的、选择性的、具有口服活性的并能穿过血脑屏障的二肽基肽酶 4 dipeptidyl peptidase 4 (DPP-4) 抑制剂。Omarigliptin 显示出抗帕金森病活性。Omarigliptin 具有改善糖尿病相关认知功能障碍的神经保护作用。

Omarigliptin (MK-3102) is a potent, selective, orally active and cross the blood-brain barrier dipeptidyl peptidase 4 (DPP-4) inhibitor. Omarigliptin shows anti-parkinsonian activity. Omarigliptinhas the neuroprotective effect to improve diabetes-associated cognitive dysfunction.

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Omarigliptin (5 mg/kg; p.o.) enhances the intestinal glucagon like peptide-1 and crosses BBB in rats.Omarigliptin (2.5, 5 mg/kg; p.o.; once a week for 8 weeks) shows anti-diabetic activity in STZ-induced diabetic mice.Omarigliptin (5 mg/kg; p.o.; daily for 28 days) shows anti-parkinsonian activity in rats.Animal Model:12 weeks, C57BL/6 male mice Dosage:2.5, 5 mg/kg Administration:P.o.; once a week for 8 weeks (50 mg/kg streptozotocin (STZ); i.p.; daily for five days)Result:Reduced the food and water intake, and caused a significant decrease in blood glucose, accompanied by increased serum insulin levels, improved insulin sensitivity and cognitive function, ameliorated diabetes-induced mitochondrial dysfunction in the brain.Animal Model:250±35 g , rats Dosage:5 mg/kg Administration:P.o.; daily for 28 days Result:Increased in brain GLP-1 concentration and passed through the BBB following oral administration.

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Proteasome/Ubiquitin

Proteasome

Proteasome | DPP-4

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1226781-44-7

398.43

C17H20F2N4O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (125.49 mM; 超声助溶 )

CS(=O)(=O)n1cc2CN(Cc2n1)[C@H]1CO[C@@H]([C@@H](N)C1)c1cc(F)ccc1F

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(-20℃)

With Ice Pack

≥ 2 years