245116-90-9
中文名稱
利多司他
英文名稱
LIDORESTAT
CAS
245116-90-9
分子式
C18H11F3N2O2S
分子量
376.35
MOL 文件
245116-90-9.mol
更新日期
2023/12/27 09:22:15
245116-90-9 結(jié)構(gòu)式
基本信息
中文別名
利多司他3-[(4,5,7-三氟-2-苯并噻唑基)甲基]-1H-吲哚-1-乙酸
英文別名
IDD-676LIDORESTAT
LIDORESTATUM
3-[(4,5,7-Trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid
[3-(4,5,7-Trifluorobenzothiazol-2-ylmethyl)indol-1-yl]acetic acid
1H-Indole-1-aceticacid, 3-[(4,5,7-trifluoro-2-benzothiazolyl)methyl]-
2-(3-((4,5,7-TRIFLUOROBENZO[D]THIAZOL-2-YL)METHYL)-1H-INDOL-1-YL)ACETIC ACID
物理化學(xué)性質(zhì)
熔點(diǎn)177-178℃
沸點(diǎn)591.4±50.0 °C(Predicted)
密度1.55
酸度系數(shù)(pKa)4.23±0.10(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見問題列表
生物活性
Lidorestat (IDD-676) 是一種有效的，選擇性的，口服活性的醛糖還原酶 (aldose reductase) 抑制劑，IC50 為 5 nM。Lidorestat 可用于慢性糖尿病并發(fā)癥。Lidorestat 還可改善神經(jīng)傳導(dǎo)并減少白內(nèi)障形成。靶點(diǎn)
IC50: 5 nM (Rldose reductase)
體外研究
From in vitro experiments, Lidorestat has a reported IC 50 against recombinant human aldose reductase (/h/-ALR2) of 5 μM. Against recombinant human aldehyde reductase (/h/-ALR1), Lidorestat has a reported IC 50 of 27,000 μM, yielding a selectivity of /h/-ALR1//h/-ALR2 of 5400:1.
體內(nèi)研究
Lidorestat (25 mg/kg/day; oral administration; twice daily; for 6 weeks; diabetic mice) treatment decreases fructose and reduces mortality in diabetic hAR-expressing mice. And Lidorestat does not affect weight.
| Animal Model: | Diabetic low-density lipoprotein (LDL) receptor-deficient [ Ldlr(-/-) ] mice |
| Dosage: | 25 mg/kg/day |
| Administration: | Oral administration; twice daily; for 6 weeks |
| Result: | Diabetic hAR-expressing mice had decreased fructose and reduced mortality. |