Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research.
体外研究
Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment significantly induceS β-cell proliferation.
Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment increases the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression.
Saxagliptin acts by preventing the degradation of glucagon-like peptide-1 and hence increases secretion of insulin and decreases secretion of glucagon.
Cell Viability Assay
Cell Line:
INS-1 832/13 cells
Concentration:
100 nM
Incubation Time:
48 hours
Result:
Significantly induced β-cell proliferation.
Western Blot Analysis
Cell Line:
INS-1 832/13 cells
Concentration:
100 nM
Incubation Time:
48 hours
Result:
Increased the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression.
体内研究
Saxagliptin (1 mg/kg; for 12 weeks) treatment in high-fat diet/streptozotocin-induced diabetic rats, significant improvement in pancreas insulin secretion capacity evaluated by hyperglycemia clamp and increased β-cell to α-cell areas ratio are observed.
Saxagliptin dose-dependently inhibits plasma DPP-4 activity in Han-Wistar rats, by ~70% at 7 hours postdose with 1 mg/kg and by ~90% at 7 hours postdose with 10 mg/kg. At 24 hours postdose, ~20% and 70% inhibition, respectively, remained.
分子式
C18H25N3O2
分子量
315.41
CAS号
361442-04-8
中文名称
沙格列汀;沙克列汀
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:
DMSO : ≥ 34 mg/mL (107.80 mM)
H2O : 10 mg/mL (31.70 mM; Need ultrasonic)
*"≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
3.1705 mL
15.8524 mL
31.7048 mL
5 mM
0.6341 mL
3.1705 mL
6.3410 mL
10 mM
0.3170 mL
1.5852 mL
3.1705 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。