Dapagliflozin ( BMS-512148 | BMS512148 | BMS 512148 )

产品货号. M14554 CAS No. 461432-26-8

一种有效的、选择性的、口服活性的 hSGLT2 抑制剂，EC50 为 1.12 nM。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
5MG	￥340	有现货
10MG	￥470	有现货
25MG	￥599	有现货
50MG	￥737	有现货
100MG	￥932	有现货
200MG	￥1239	有现货
500MG	获取报价	有现货
1G	获取报价	有现货

产品询价大包装询价加入购物车

生物学信息

产品名称

Dapagliflozin
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

一种有效的、选择性的、口服活性的 hSGLT2 抑制剂，EC50 为 1.12 nM。
产品描述

A potent, selective, orally active hSGLT2 inhibitor with EC50 of 1.12 nM; displays >300-fold selectivity over hSGLT1 (EC50=330 nM), highly selectivity versus GLUT transporters; also is a potent selective inhibitor of rSGLT2 (EC50=3 nM), with 200-fold selectivity versus rSGLT1; significantly improves glucose homeostasis, reduces blood glucose levels in hyperglycemic streptozotocin (STZ) rats.Diabetes Approved(In Vitro):Dapagliflozin (0-10 μM；24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner.Dapagliflozin (0-10 μM；2 hours) increases the HIF1 expression, increases AMPK and EKR phosphorylation in hypoxic HK2 cells, but shows no effect on the phosphorylation of AMPK and ERK in normoxic HK2 cells..(In Vivo):Dapagliflozin (oral administration; 10 mg/kg) causes a marked increase in urinary glucose in SGLT2i-mice, suppresses BAT thermogenesis by reducing sympathetic nerve activity and enhances hepatic gluconeogenesis and glycogenolysis.
体外实验

Dapagliflozin (0-10 μM；24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner.Dapagliflozin (0-10 μM；2 hours) increases the HIF1 expression, increases AMPK and EKR phosphorylation in hypoxic HK2 cells, but shows no effect on the phosphorylation of AMPK and ERK in normoxic HK2 cells.Cell Viability Assay Cell Line:Hypoxic HK2 cells Concentration:0 μM, 1 μM, 2 μM, 5 μM, 10 μM Incubation Time:24 hours Result:Improved the cell viability in a dose-dependent manner compared with control cells.Western Blot Analysis Cell Line:Hypoxic HK2 cells, Normoxic HK2 cells Concentration:0 μM, 1 μM, 2 μM, 5 μM, 10 μM Incubation Time:24 hours Result:Induced HIF1 expression in hypoxic and normoxic HK2 cells.
体内实验

Dapagliflozin (oral administration; 10 mg/kg) causes a marked increase in urinary glucose in SGLT2i-mice, suppresses BAT thermogenesis by reducing sympathetic nerve activity and enhances hepatic gluconeogenesis and glycogenolysis.
同义词

BMS-512148 | BMS512148 | BMS 512148
通路

GPCR/G Protein
靶点

SGLT
受体

hSGLT2
研究领域

Metabolic Disease
适应症

Diabetes

化学信息

CAS Number

461432-26-8
分子量

408.8726
分子式

C21H25ClO6
纯度

>98% (HPLC)
溶解度

10 mM in DMSO
SMILES

O[C@H]1[C@H](C2=CC=C(Cl)C(CC3=CC=C(OCC)C=C3)=C2)O[C@H](CO)[C@@H](O)[C@@H]1O
化学全称

D-Glucitol, 1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-, (1S)-

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

参考文献

1. Meng W, et al. J Med Chem. 2008 Mar 13;51(5):1145-9. 2. Han S, et al. Diabetes. 2008 Jun;57(6):1723-9. 3. Wilson C. Nat Rev Endocrinol. 2010 Oct;6(10):531. 4. Komoroski B, et al. Clin Pharmacol Ther. 2009 May;85(5):513-9.

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摩尔计算器

分子量计算器

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