您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Saxagliptin hydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Saxagliptin hydrochloride
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。
Saxagliptin hydrochloride图片
CAS NO:709031-78-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
BMS-477118 hydrochloride
产品介绍
Saxagliptin hydrochloride (BMS-477118 hydrochloride) 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) (Ki= 0.6-1.3 nM) 抑制剂。Saxagliptin hydrochloride 可用于 2 型糖尿病的研究。
生物活性

Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally activedipeptidyl peptidase-4 (DPP-4)(Ki= 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride 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

351.87

Formula

C18H26ClN3O2

CAS 号

709031-78-7

中文名称

盐酸沙格列汀;盐酸沙克列汀

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.