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CAS No.: 1191995-00-2

Dorzagliatin Catalog No. CSN20177

Synonyms: HMS5552;sinogliatin;RO-5305552

Dorzagliatin is a glucokinase activator on glucose metabolism.

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技术信息

生物活性

描述Glucokinase (GK) is a key regulatory enzyme in whole-body glucose homeostasis. Dorzagliatin is a novel GK activator that has been shown to decrease blood glucose levels and improves GK activity and insulin resistance. Two hours after a single intragastric administration of 10 mg/kg or 30 mg/kg dorzagliatin decreased glucose levels in diabetic rats by ~25% and 31%, respectively, compared with the levels measured before dorzagliatin treatment. After 27 days of treatment, a significant reduction in fasting plasma glucose levels was observed in dorzagliatin-treated diabetic rats compared to the vehicle-treated group. Also, rats administered with 10 mg/kg or 30 mg/kg dorzagliatin showed a reduction in glucose levels (~18% and 23%, respectively) measured 2h after HMS5552 administration compared with the levels detected before dorzagliatin administration. Treatment of diabetic rats with 10 mg/kg and 30 mg/kg dorzagliatin also significantly decreased the levels of fasting insulin compared with the diabetic group. Rats treated with dorzagliatin (10 mg/kg and 30 mg/kg) for one months showed significantly decreased K_m value of GK (5.9 ± 0.43mmol/L and 5.6 ± 0.27mmol/L, respectively) compared to the diabetic group (9.9 ± 0.55mmol/L). After dorzagliatin treatment, the number of GK- and insulin-immunopositive cells was also significantly increased in diabetic rats. The protein and mRNA expressions of GK in dorzagliatin-treated rats were significantly higher than those observed in the diabetic group.^[3]
作用机制Dorzagliatin is a fourth-generation GK activator with a structurally novel amino-acid-based chemical scaffold, which improves GK activity in a rat model of T2DM induced by a high-fat diet and streptozotocin.^[3]
参考文献

[1] Wang P, Liu H, et al. Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus. J Diabetes Res. 2017;2017:5812607.
[2] Xu H, Sheng L, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of novel glucokinase activator HMS5552: results from a first-in-human single ascending dose study. Drug Des Devel Ther. 2016 May 9;10:1619-26.
[3] Wang P, Liu H, Chen L, Duan Y, Chen Q, Xi S. Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus. J Diabetes Res. 2017;2017:5812607. doi:10.1155/2017/5812607

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
- 2.1602 mL
- 10.8008 mL
- 21.6017 mL
- 5 mM
- 0.4320 mL
- 2.1602 mL
- 4.3203 mL
- 10 mM
- 0.2160 mL
- 1.0801 mL
- 2.1602 mL

技术信息

CAS号

1191995-00-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H27ClN4O5

运输

蓝冰

分子量

462.93

别名

HMS5552;sinogliatin;RO-5305552

溶解度

DMSO	91.0 mg/mL (196.6 mM)
Water	Insoluble
Ethanol	92.0 mg/mL (198.7 mM)

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