147254-64-6
147254-64-6 結構式
基本信息
AS 3201
SX-3201
Raniestat
Ranirestat
AS-3201
SX-3201
Ranirestat,AS-3201
Ranirestat >=97% (HPLC)
(3R)-2'-(4-Bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'-1'H-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone
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)-
物理化學性質(zhì)
常見問題列表
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. |