| Bioactivity | 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. Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction[1][2][3]. | ||||||||||||
| In Vivo | Omarigliptin (5 mg/kg; p.o.) enhances the intestinal glucagon like peptide-1 and crosses BBB in rats[1].Omarigliptin (2.5, 5 mg/kg; p.o.; once a week for 8 weeks) shows anti-diabetic activity in STZ-induced diabetic mice[2].Omarigliptin (5 mg/kg; p.o.; daily for 28 days) shows anti-parkinsonian activity in rats[3]. Animal Model: | ||||||||||||
| Name | Omarigliptin | ||||||||||||
| CAS | 1226781-44-7 | ||||||||||||
| Formula | C17H20F2N4O3S | ||||||||||||
| Molar Mass | 398.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ayoub BM, et al. Repositioning of Omarigliptin as a once-weekly intranasal Anti-parkinsonian Agent. Sci Rep. 2018 Jun 12;8(1):8959. [2]. Li X, et al. Omarigliptin alleviates cognitive dysfunction in Streptozotocin-induced diabetic mouse. Bioengineered. 2022 Apr;13(4):9387-9396. [3]. Ayoub BM, et al. Repurposing of Omarigliptin as a Neuroprotective Agent Based on Docking with A2A Adenosine and AChE Receptors, Brain GLP-1 Response and Its Brain/Plasma Concentration Ratio after 28 Days Multiple Doses in Rats Using LC-MS/MS. Molecules. 2 |