Zenarestat | Aldose reductase inhibitor | Probechem Biochemicals

Chemical Structure : Zenarestat

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Zenarestat (FR-74366, FR74366, FK-366)

货号: PC-25939Not For Human Use, Lab Use Only.

Zenarestat (FK-366, FR-74366) is a highly potent, reversible, and mixed type inhibitor of aldose reductase (AR) with IC50 of 3.6 and 4.4 nM for purified AR from the rat sciatic nerve and rat lens.

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生物&药学活性

Zenarestat (FK-366, FR-74366) is a highly potent, reversible, and mixed type inhibitor of aldose reductase (AR) with IC50 of 3.6 and 4.4 nM for purified AR from the rat sciatic nerve and rat lens.
Zenarestat (FK-366, FR-74366) inhibited sorbitol accumulation in the isolated human erythrocyte (IC50 = 1.6 mumol/L), rat lens (IC50 = 39 mumol/L), and rat sciatic nerve (IC50 = 17 mumol/L) incubated with high glucose concentrations.
Oral administration of FR74366 to streptozotocin (STZ)-induced diabetic rats for 2 weeks decreased sorbitol levels (ED50 = 3.7 mg/kg for sciatic nerve, 23 mg/kg for lens, 52 mg/kg for retina, and 62 mg/kg for renal cortex).
Zenarestat (FK-366, FR-74366) induced recovery of reduced motor nerve conduction velocity in diabetic rats, correlated well with reduction of accumulated sorbitol and fructose levels and normalization of decreased myoinositol levels.

物理化学性质&存储条件

分子量	441.64
分子式	C17H11BrClFN2O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(3-(4-Bromo-2-fluorobenzyl)-7-chloro-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)acetic acid

参考文献

1. Ao S, et al. Metabolism. 1991 Jan;40(1):77-87.

2. Akagi Y, et al. Nippon Ganka Gakkai Zasshi. 1989 Apr;93(4):494-500.

Zenarestat (FR-74366, FR74366, FK-366)

生物&药学活性

物理化学性质&存储条件

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Zenarestat (FR-74366, FR74366, FK-366)

生物&药学活性

物理化学性质&存储条件

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