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

基本信息物理化學(xué)性質(zhì) 安全數(shù)據(jù) 圖譜信息雷尼司他價(jià)格(試劑級) 常見問題列表

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(dòng)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

旋光度 (Optical Rotation)[α]/D -5 to -10°, c =1.0 in methanol

InChI1S/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

InChIKeyQCVNMNYRNIMDKV-QGZVFWFLSA-N

SMILESO=C(N1CC2=C(F)C=C(Br)C=C2)C3=CC=CN3[C@@]4(CC(NC4=O)=O)C1=O

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS) 有害 (GHS07)

GHS07

警示詞警告

危險(xiǎn)性描述H315-H319-H335

防范說明P261-P264-P271-P280-P302+P352-P305+P351+P338

WGK GermanyWGK 3

存儲類別11 - Combustible Solids

危險(xiǎn)性類別Eye Irrit. 2
Skin Irrit. 2
STOT SE 3

圖譜信息

雷尼司他(147254-64-6)核磁圖(¹HNMR)

雷尼司他價(jià)格(試劑級)

報(bào)價(jià)日期	產(chǎn)品編號	產(chǎn)品名稱	CAS號	包裝	價(jià)格
2026/06/05	HY-15314	雷尼司他 Ranirestat	147254-64-6	1 mg	1181元
2026/06/05	HY-15314	雷尼司他 Ranirestat	147254-64-6	5mg	2600元
2026/06/05	HY-15314	雷尼司他 Ranirestat	147254-64-6	10mM * 1mLin DMSO	2860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(dòng)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.