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141200-24-0

中文名称 达格列酮
英文名称 darglitazone
CAS 141200-24-0
分子式 C23H20N2O4S
分子量 420.48
MOL 文件 141200-24-0.mol
更新日期 2023/03/17 20:03:07
141200-24-0 结构式 141200-24-0 结构式

基本信息

中文别名
达格列酮
英文别名
darglitazone
2,4-Thiazolidinedione, 5-[[4-[3-(5-methyl-2-phenyl-4-oxazolyl)-1-oxopropyl]phenyl]methyl]-
5-[[4-[3-(5-methyl-2-phenyl-1,3-oxazol-4-yl)propanoyl]phenyl]methyl]-1,3-thiazolidine-2,4-dione

物理化学性质

储存条件-20°C储存
溶解度DMSO:20.0(Max Conc. mg/mL);47.56(Max Conc. mM)
DMF:20.0(Max Conc. mg/mL);47.56(Max Conc. mM)
形态结晶固体

常见问题列表

生物活性
Darglitazone (CP-86325),一种噻唑烷二酮,是一种有效的,选择性的和具有口服活性的 PPAR-γ 激动剂。Darglitazone 有效控制血糖和脂质代谢,可用于 II 型糖尿病研究。
靶点

PPAR-γ

体外研究

In cell lines representing white (3T3-L1 and 3T3-F442A) and brown (HIB-1B) adipose tissues and skeletal muscle (L6), within 4 h of exposing these cells to 30 μM Darglitazone, there is an increase in uncoupling protein 2 (UCP2) mRNA which reached a plateau of 5-10 times the basal in about 8 h. Darglitazone can stimulate the expression of UCP2 gene probably via PPAR-γ.

体内研究

Darglitazone treatment restores euglycemia and normalized elevated corticosterone, triglycerides, and very-low-density lipoprotein levels. Darglitazone dramatically reduces the infarct size in the ob/ob mice at 24 h of recovery. Darglitazone treatment restores acute cerebral inflammatory responses that were absent in the diabetic mice and profoundly improved their recovery from hypoxic-ischemic (H/I) insult.

Animal Model: Male diabetic ob/ob mice
Dosage: 1 mg/kg
Administration: Oral administration; daily; for 7 days
Result: Normalized blood glucose and reduced circulating triglycerides (TG) and very-low-density lipoproteins (VLDL) in diabetic ob/ob mice without having any effect in the nondiabetic mice.
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