| 生物活性 |
Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin . Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
|
||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 分子式 |
C16H9D6F6N5O
|
||||||||||||
| 分子量 |
413.35
|
||||||||||||
| CAS号 |
1133211-99-0
|
||||||||||||
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
||||||||||||
| 储存方式 |
|
咨询热线：
400-881-9290
Data Sheet
