利多司他
| 中文名称 | 利多司他 |
|---|---|
| 中文同义词 | 利多司他;3-[(4,5,7-三氟-2-苯并噻唑基)甲基]-1H-吲哚-1-乙酸;化合物 T15756 |
| 英文名称 | LIDORESTAT |
| 英文同义词 | LIDORESTAT;1H-Indole-1-aceticacid, 3-[(4,5,7-trifluoro-2-benzothiazolyl)methyl]-;[3-(4,5,7-Trifluorobenzothiazol-2-ylmethyl)indol-1-yl]acetic acid;3-[(4,5,7-Trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid;2-(3-((4,5,7-TRIFLUOROBENZO[D]THIAZOL-2-YL)METHYL)-1H-INDOL-1-YL)ACETIC ACID;LIDORESTATUM;IDD-676;(VOI)LIDORESTAT |
| CAS号 | 245116-90-9 |
| 分子式 | C18H11F3N2O2S |
| 分子量 | 376.35 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 245116-90-9.mol |
| 结构式 |  |
利多司他 性质
| 熔点 | 177-178℃ |
|---|---|
| 沸点 | 591.4±50.0 °C(Predicted) |
| 密度 | 1.55 |
| 形态 | 固体 |
| 酸度系数(pKa) | 4.23±0.10(Predicted) |
| 颜色 | 浅黄至黄色 |
Lidorestat (IDD-676) 是一种有效的，选择性的，口服活性的醛糖还原酶 (aldose reductase) 抑制剂，IC50 为 5 nM。Lidorestat 可用于慢性糖尿病并发症。Lidorestat 还可改善神经传导并减少白内障形成。
IC50: 5 nM (Rldose reductase)
From in vitro experiments, Lidorestat has a reported IC 50 against recombinant human aldose reductase (/h/-ALR2) of 5 μM. Against recombinant human aldehyde reductase (/h/-ALR1), Lidorestat has a reported IC 50 of 27,000 μM, yielding a selectivity of /h/-ALR1//h/-ALR2 of 5400:1.
Lidorestat (25 mg/kg/day; oral administration; twice daily; for 6 weeks; diabetic mice) treatment decreases fructose and reduces mortality in diabetic hAR-expressing mice. And Lidorestat does not affect weight.
| Animal Model: | Diabetic low-density lipoprotein (LDL) receptor-deficient [ Ldlr(-/-) ] mice |
| Dosage: | 25 mg/kg/day |
| Administration: | Oral administration; twice daily; for 6 weeks |
| Result: | Diabetic hAR-expressing mice had decreased fructose and reduced mortality. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-106198 | Lidorestat | 5 mg | 500元 | |
| 2024/08/19 | HY-106198 | 利多司他 Lidorestat | 245116-90-9 | 10mM * 1mLin DMSO | 550元 |