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CAS No.: 960404-48-2

Dapagliflozin ((2S)-1,2-propanediol, hydrate)/达格列净一水丙二醇 Catalog No. CSN13871

Synonyms: BMS-512148 (2S)-1,2-propanediol, hydrate;BMS-512148 (2S)-1,2-Propanediol Hydrate;Dapagliflozin ((2S)-1,2-propanediol

Dapagliflozin propanediol is an inhibitor of SGLT2 that is used for the treatment of of type 2 diabetes mellitus.

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技术信息

生物活性

描述The sodium-dependent glucose transport (SGLT) proteins belong to the sodium glucose cotransporter family. Sodium-dependent glucose transport 2 (SGLT2) is a high-capacity, low-affinity transporter that is expressed mainly in the kidney. It has a Na(+) to glucose coupling ratio of 1:1. It is estimated that 90% of renal glucose reabsorption is facilitated by SGLT2 residing on the surface of the epithelial cells lining the S1 segment of the proximal tubule. Dapagliflozin Propanediol Hydrate is the propanediol hydrate form of Dapagliflozin. Dapagliflozin is a potent and selective SGLT2 inhibitor. In an experiment system of Chinese hamster ovary cells stably expressing human SGLT2 and SGLT1, data yielded by monitoring inhibition of AMG showed that the EC50 of dapagliflozin for human SGLT2 inhibition was 1.1 nM, while that for human SGLT1 was 1390 nM. In acute normal and diabetic rat studies, SD or ZDF rats were dosed orally with single doses of dapagliflozin at 0.01 mg/kg, 0.1 mg.kg, 1 mg/kg or 10 mg/kg. In normal rats， the results were that dapagliflozin caused significant dose-dependent glucosuria and increase in urine volume, with 1 mg/kg producing a 400-fold increase in urine glucose and a threefold increase in urine volume versus vehicle over 24 h post-dose. Dapagliflozin administration was also associated with a reduction in glucose area under the curve over 1 h post-dose at 1 and 10 mg/kg doses in the glucose tolerance test in normal rats. In ZDF rats, dapagliflozin dose-dependently increased urine glucose and urine volume excretion at 6 h post-dose . In another study, dapagliflozin was administrated at the dose of 0.5 mg/kg orally once daily for 15 days. When measured 24 h after the final dose on day 15, ZDF rats treated with dapagliflozin displayed a 53% decrease in 18-h FPG level compared with vehicle-treated rats.
参考文献

[1] Ghosh RK, Ghosh SM, et al. SGLT2 inhibitors: a new emerging therapeutic class in the treatment of type 2 diabetes mellitus. J Clin Pharmacol. 2012 Apr;52(4):457-63.
[2] Hussar DA, Purzycki DJ. Dapagliflozin propanediol, avanafil, and conjugated estrogens/bazedoxifene. J Am Pharm Assoc (2003). 2014 May-Jun;54(3):314; 316-8.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9881 mL
- 9.9407 mL
- 19.8814 mL
- 5 mM
- 0.3976 mL
- 1.9881 mL
- 3.9763 mL
- 10 mM
- 0.1988 mL
- 0.9941 mL
- 1.9881 mL

技术信息

CAS号

960404-48-2

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H35ClO9

运输

蓝冰

分子量

502.98

别名

BMS-512148 (2S)-1,2-propanediol, hydrate;BMS-512148 (2S)-1,2-Propanediol Hydrate;Dapagliflozin ((2S)-1,2-propanediol;hydrate)Dapagliflozin ((2S)-1,2-propanediol;hydrate);BMS-512148 (2S)-1,2-propanediol;hydrate;Dapagliflozin Propanediol Monohydrate;达格列净一水丙二醇

溶解度

DMSO	99.0 mg/mL (196.8 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (198.8 mM)

动物实验配方

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Dapagliflozin ((2S)-1,2-propanediol, hydrate)/达格列净一水丙二醇 Catalog No. CSN13871

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