Omarigliptin B

Research use only, not for human use.

Omarigliptin is a potent and selective oral dipeptidyl peptidase 4 (DPP4) inhibitor with IC50 value of 1.6 nM.

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.

——

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.

——

Proteasome/Ubiquitin

Proteasome

Proteasome | DPP-4

——

——

1226781-44-7

398.43

C17H20F2N4O3S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (125.49 mM; Ultrasonic )

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

——

(-20℃)

With Ice Pack

≥ 2 years