雷尼司他

生物活性靶点体外研究体内研究雷尼司他试剂级价格

雷尼司他

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
中文名:雷尼司他
CBNumber:CB72589748
分子式:C17H11BrFN3O4
分子量:420.19
MOL File:147254-64-6.mol

雷尼司他化学性质

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
酸度系数(pKa) :10.48±0.20(Predicted)
形态 :Solid
颜色 :Off-white to pink

雷尼司他性质、用途与生产工艺

生物活性 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。
靶点

IC50: 11 nM (Rat lens aldose reductase) and 15 nM (Recombinant humanaldose reductase)
Ki: 0.38 nM (Recombinant humanaldose reductase)
体外研究

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.

体内研究

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.