雷尼司他
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- CAS号:
- 147254-64-6
- 英文名:
- (3R)-2'-(4-Bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'-1'H-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone
- 英文别名:
- AS-3201;AS 3201;SX-3201;Raniestat;Ranirestat;AS-3201; SX-3201;Ranirestat,AS-3201;Ranirestat >=97% (HPLC);(R)-2'-(4-bromo-2-fluorobenzyl)-1'H-spiro[pyrrolidine-3,4'-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone;(3R)-2'-(4-Bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'-1'H-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone
- 中文名:
- 雷尼司他
- 中文别名:
- 雷尼司他;化合物 T16723;(R)-2'-(4-BROMO-2-FLUOROBENZYL)-1'H-SPIRO[PYRROLIDINE-3,4'-PYRROLO[1,2-A]PYRAZINE]-1',2,3',5(3'H)-TETRAONE
- CBNumber:
- CB72589748
- 分子式:
- C17H11BrFN3O4
- 分子量:
- 420.19
- MOL File:
- 147254-64-6.mol
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雷尼司他化学性质
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熔点:
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192-193℃
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沸点:
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702.7±60.0 °C(Predicted)
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密度:
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1.83
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储存条件:
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Sealed in dry,Store in freezer, under -20°C
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酸度系数(pKa):
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10.48±0.20(Predicted)
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雷尼司他性质、用途与生产工艺
Ranirestat (AS-3201) 是一种有效的,口服活性的醛糖还原酶 (AR) 抑制剂,对大鼠晶状体 AR 和重组人 AR 的 IC50 分别为 11 nM 和 15 nM,对于重组人 AR 的 Ki 为 0.38 nM。Ranirestat 可用于糖尿病感觉运动性多发性神经病的研究,并且对糖尿病视网膜具有神经保护作用。
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:
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Male STD-Wistar rats aged about (12-week-old; 260-290 g) injected with Streptozotocin (STZ)
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Dosage:
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0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
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Administration:
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Oral administration; once daily; for 3 weeks
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Result:
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Dose-dependently decreased the elevated sorbitol and fructose levels in the rat sciatic nerves without affecting blood glucose level.
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雷尼司他
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/01/25 | HY-15314 | Ranirestat | | 1 mg | 1181元 |
2024/01/25 | HY-15314 | 雷尼司他 Ranirestat | 147254-64-6 | 5mg | 2600元 |
147254-64-6, 雷尼司他 相关搜索:
- C17H11BrFN3O4
- 化合物 T16723
- (R)-2'-(4-BROMO-2-FLUOROBENZYL)-1'H-SPIRO[PYRROLIDINE-3,4'-PYRROLO[1,2-A]PYRAZINE]-1',2,3',5(3'H)-TETRAONE
- 雷尼司他
- 147254-64-6
- (R)-2'-(4-bromo-2-fluorobenzyl)-1'H-spiro[pyrrolidine-3,4'-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone
- Ranirestat >=97% (HPLC)
- SX-3201
- AS-3201; SX-3201
- Raniestat
- Ranirestat,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)-
- AS-3201
- AS 3201
- Ranirestat
- (3R)-2'-(4-Bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'-1'H-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone