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147254-64-6

中文名稱 雷尼司他
英文名稱 (3R)-2'-(4-Bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'-1'H-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone
CAS 147254-64-6
分子式 C17H11BrFN3O4
分子量 420.19
MOL 文件 147254-64-6.mol
更新日期 2024/12/03 15:40:32
147254-64-6 結(jié)構(gòu)式 147254-64-6 結(jié)構(gòu)式

基本信息

中文別名
雷尼司他
英文別名
AS-3201
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)-
所屬類別
生物化工：激動劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)192-193℃
沸點(diǎn)702.7±60.0 °C(Predicted)
密度1.83
儲存條件Sealed in dry,Store in freezer, under -20°C
溶解度DMSO: 20mg/mL, clear
酸度系數(shù)(pKa)10.48±0.20(Predicted)
形態(tài)Solid
顏色Off-white to pink
旋光性 (optical activity)[α]/D -5 to -10°, c =1.0 in methanol

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H319-H335
雷尼司他價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/02/08HY-15314雷尼司他
Ranirestat		147254-64-61 mg1181元
2025/02/08HY-15314雷尼司他
Ranirestat		147254-64-65mg2600元
2025/02/08HY-15314雷尼司他
Ranirestat		147254-64-610mM * 1mLin DMSO2860元

常見問題列表

生物活性
Ranirestat (AS-3201) 是一種有效的，口服活性的醛糖還原酶 (AR) 抑制劑，對大鼠晶狀體 AR 和重組人 AR 的 IC50 分別為 11 nM 和 15 nM，對于重組人 AR 的 Ki 為 0.38 nM。Ranirestat 可用于糖尿病感覺運(yùn)動性多發(fā)性神經(jīng)病的研究，并且對糖尿病視網(wǎng)膜具有神經(jīng)保護(hù)作用。
靶點(diǎn)

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

體外研究

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.

體內(nèi)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.
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