Factory Supply Raw Material Powder API Mk-3102 CAS 1226781-44-7 Omarigliptin

Superiority:

English name: Omarigliptin (MK-3102)

CAS number: 1226781-44-7

Molecular formula: C17H20F2N4O3S

Molecular weight: 398.43

EINECS Number: 682-558-0

Boiling point: 529.4±60.0°C (Predicted)

Density: 1.61±0.1g/cm3(Predicted)

Storage conditions: 2-8°C (protect from light)

Acidity coefficient (pKa): 9.11±0.60 (Predicted)

Octagliptin (MK-3102) is an ultra-long-acting dipeptidyl peptidase-4 (DPP-4) inhibitor oral hypoglycemic agent developed by Merck & Co. -4 inhibitory effect, has a new hypoglycemic mechanism, and has the advantages of not gaining weight, not causing hypoglycemia, and not causing edema. Its mechanism of action is to prolong the action time of GLP-1 by inhibiting the degradation of glucagon-like peptide-1 (GLP-1) by DPP-4 enzyme in vivo, thereby increasing the levels of endogenous GLP-1 and GIP in the blood. concentration and ultimately improve glycemic control. GLP-1 is a kind of incretin, which is a kind of medium-length linear polypeptide hormone with insulin secretion-stimulating effect produced in the intestine. Its function characteristics include: it is only produced after meals, and it promotes the secretion of insulin from pancreatic β cells, thereby reducing the blood sugar, does not induce hypoglycemia; inhibits islet α-cell secretion of glucagon; delays gastric emptying to facilitate postprandial blood glucose control; inhibits intestinal secretion of lipoproteins and may reduce postprandial hyperglycemia as a risk factor for cardiovascular disease blood lipids, thus having a cardioprotective effect. Octagliptin, a once-weekly DPP-4 inhibitor oral hypoglycemic agent, improves medication compliance. Poor medication adherence is a common problem in clinical practice, especially in chronic asymptomatic diseases such as type 2 diabetes, dyslipidemia, and hypertension. In patients with type 2 diabetes, improving medication adherence is essential to maintain good glycemic control during long-term treatment, thereby preventing the exacerbation of type 2 diabetes and the occurrence and progression of complications. On September 19, 2014, Merck announced the first data from the Phase 3 clinical development program of omarigliptin in the treatment of type 2 diabetes at the 50th European Association of Diabetes (EASD) annual meeting. Compared with placebo, omarigliptin significantly reduced glycated hemoglobin (HbA1c) levels, while with a once-daily dose of 50 mg (standard starting dose in Japan) DPP-4 inhibitor Januvir (Januvir, sitagliptin) Equivalent efficacy and tolerability. In December 2014, Merck submitted a New Drug Application (NDA) for the experimental hypoglycemic drug omarigliptin to Japan's Pharmaceuticals and Medical Devices Agency (PMDA), marking the world's first regulatory application.

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