达格列酮

生物活性靶点体外研究体内研究达格列酮试剂级价格

达格列酮

CAS号:141200-24-0
英文名:darglitazone
中文名:达格列酮
CBNumber:CB41382639
分子式:C23H20N2O4S
分子量:420.48
MOL File:141200-24-0.mol

达格列酮化学性质

密度 :1.306±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
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 :A crystalline solid
酸度系数(pKa) :6.22±0.50(Predicted)
颜色 :White to light yellow

达格列酮性质、用途与生产工艺

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.