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141200-24-0

中文名稱 達格列酮
英文名稱 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 結(jié)構(gòu)式 141200-24-0 結(jié)構(gòu)式

基本信息

中文別名
達格列酮
英文別名
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

物理化學性質(zhì)

密度1.306±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
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)
酸度系數(shù)(pKa)6.22±0.50(Predicted)
形態(tài)結(jié)晶固體
顏色White to light yellow

常見問題列表

生物活性
Darglitazone (CP-86325),一種噻唑烷二酮,是一種有效的,選擇性的和具有口服活性的 PPAR-γ 激動劑。Darglitazone 有效控制血糖和脂質(zhì)代謝,可用于 II 型糖尿病研究。
靶點

PPAR-γ

體外研究

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.

體內(nèi)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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