达格列酮
| 中文名称 | 达格列酮 |
|---|---|
| 中文同义词 | 达格列酮;化合物 T22708 |
| 英文名称 | darglitazone |
| 英文同义词 | 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;oral,UCP2,corticosterone,PPAR-γ,CP86325,Darglitazone,Diabetes,CP-86325,Inhibitor,PPAR,inhibit,Peroxisome proliferator-activated receptors,CP 86325,thiazolidinedione |
| CAS号 | 141200-24-0 |
| 分子式 | C23H20N2O4S |
| 分子量 | 420.48 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 141200-24-0.mol |
| 结构式 |  |
达格列酮 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(最大浓度 mg/mL);47.56(最大浓度 mM) DMF:20.0(最大浓度 mg/mL);47.56(最大浓度 mM) |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 6.22±0.50(Predicted) |
|
PPAR-γ
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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.
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. |