雷尼司他
| 中文名称 | 雷尼司他 |
|---|---|
| 中文同义词 | 雷尼司他;(R)-2'-(4-BROMO-2-FLUOROBENZYL)-1'H-SPIRO[PYRROLIDINE-3,4'-PYRROLO[1,2-A]PYRAZINE]-1',2,3',5(3'H)-TETRAONE;化合物 T16723 |
| 英文名称 | (3R)-2'-(4-Bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'-1'H-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone |
| 英文同义词 | AS-3201; SX-3201;SX-3201;(3R)-2'-(4-Bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'-1'H-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone;Ranirestat;AS 3201;AS-3201;Spiro[pyrrolidine-3,4'(1'H)-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetrone,2'-[(4-broMo-2-fluorophenyl)Methyl]-, (3R)-;Ranirestat,AS-3201 |
| CAS号 | 147254-64-6 |
| 分子式 | C17H11BrFN3O4 |
| 分子量 | 420.19 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 147254-64-6.mol |
| 结构式 |  |
雷尼司他 性质
| 熔点 | 192-193℃ |
|---|---|
| 沸点 | 702.7±60.0 °C(Predicted) |
| 密度 | 1.83 |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | DMSO: 20mg/mL, clear |
| 酸度系数(pKa) | 10.48±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 米白色至粉红色 |
| 旋光度 (Optical Rotation) | [α]/D -5 to -10°, c =1.0 in methanol |
| InChI | 1S/C17H11BrFN3O4/c18-10-4-3-9(11(19)6-10)8-21-14(24)12-2-1-5-22(12)17(16(21)26)7-13(23)20-15(17)25/h1-6H,7-8H2,(H,20,23,25)/t17-/m1/s1 |
| InChIKey | QCVNMNYRNIMDKV-QGZVFWFLSA-N |
| SMILES | O=C(N1CC2=C(F)C=C(Br)C=C2)C3=CC=CN3[C@@]4(CC(NC4=O)=O)C1=O |
IC50: 11 nM (Rat lens aldose reductase) and 15 nM (Recombinant humanaldose reductase)
Ki: 0.38 nM (Recombinant humanaldose reductase)
Ranirestat concentration-dependently inhibits sorbitol accumulation in rat erythrocytes and sciatic nerves incubated in the high concentration (500 mg/dl) of glucose. The potency of Ranirestat inhibition of sorbitol accumulation is similar between rat erythrocytes and sciatic nerves with IC 50 values of 0.010 μM and 0.041 μM, respectively.
Ranirestat (0.03-1.0 mg/kg; oral administration; once daily; for 3 weeks; male STD-Wistar rats) treatment dose-dependently decreases the elevated sorbitol and fructose levels in the rat sciatic nerves without affecting blood glucose level. Ranirestat also improves the STZ-induced decrease in motor nerve conduction velocity (MNCV) in a dose-dependent manner.
| Animal Model: | Male STD-Wistar rats aged about (12-week-old; 260-290 g) injected with Streptozotocin (STZ) |
| Dosage: | 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg |
| Administration: | Oral administration; once daily; for 3 weeks |
| Result: | Dose-dependently decreased the elevated sorbitol and fructose levels in the rat sciatic nerves without affecting blood glucose level. |
安全信息
| WGK Germany | WGK 3 |
|---|---|
| 存储类别 | 11 - 可燃固体 |
| 危险性类别 | 眼部刺激 类别2 经皮刺激 类别2 特异性靶器官毒性-一次接触，类别3 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-15314 | 雷尼司他 Ranirestat | 147254-64-6 | 1 mg | 1181元 |
| 2025/12/22 | HY-15314 | 雷尼司他 Ranirestat | 147254-64-6 | 5mg | 2600元 |