| CAS NO: | 1226781-44-7 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1226781-44-7 |
| 别名 | 奥格列汀（MK-3102）,MK-3102 |
| 化学名 | (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine |
| Canonical SMILES | CS(N1C=C2CN([C@](CO3)([H])C[C@@](N)([H])[C@@]3([H])C4=C(F)C=CC(F)=C4)CC2=N1)(=O)=O |
| 分子式 | C17H20F2N4O3S |
| 分子量 | 398.43 |
| 溶解度 | ≥ 17.15mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Dipeptidyl peptidase IV (DPP-4) inhibitors improve glycemic control in patients with type 2 diabetes by prolonging the half-life of incretin peptides, which stimulate insulin secretion and decrease glucagon release in a glucose-dependent manner. MK-3102 is a novel long-acting DPP-4 inhibitor. In vitro: MK-3102 is a competitive, reversible inhibitor of DPP-4 and is more potent than sitagliptin. It is highly selective over all proteases tested, including QPP, FAP, PEP, DPP8, and DPP9. The compound has weak ion channel activity [1]. In vivo: MK-3102 was evaluated for its ability to improve glucose tolerance in lean mice. When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test, it significantly reduced blood glucose excursion in a dosedependent manner from 0.01 mg/kg to 0.3 mg/kg [1]. Clinical trial: MK-3102 is currently in phase 3 clinical trial for type 2 diabetes mellitus. Dose-dependent efficacy in 2 h post meal glucose reduction, fasting plasma glucose reduction, and HbA1c and safety profile similar to that seen with once daily DPP-4 inhibitor such as sitagliptin was observed in a 12-week phase IIB dose-rangefinding study [1]. Reference: |
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