Saxagliptin

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Saxagliptin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

361442-04-8

沙格列汀
BMS-477118

Saxagliptin (BMS-477118) 是一种有效，选择性，可逆，竞争性和具有口服活性的二肽基肽酶 4 (DPP-4) (K_i= 0.6-1.3 nM) 抑制剂。Saxagliptin 可用于 2 型糖尿病的研究。

生物活性

Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally activedipeptidyl peptidase-4 (DPP-4)(K_i= 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research^[1]^[2]^[3].

IC₅₀& Target

Ki: 0.6-1.3 nM (Dipeptidyl peptidase-4 (DPP-4))^[2]

体外研究
(In Vitro)

Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment significantly induceS β-cell proliferation^[1].
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^[1].
Saxagliptin acts by preventing the degradation of glucagon-like peptide-1 and hence increases secretion of insulin and decreases secretion of glucagon^[3].

Cell Viability Assay^[1]

Cell Line:	INS-1 832/13 cells
Concentration:	100 nM
Incubation Time:	48 hours
Result:	Significantly induced β-cell proliferation.

Western Blot Analysis^[1]

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
(In Vivo)

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^[1].
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^[2].

Clinical Trial

分子量

315.41

性状

Solid

Formula

C₁₈H₂₅N₃O₂

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℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 8.33 mg/mL (26.41 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。