化学数据
分子量分子式CAS号储存条件
678.48
C20H34AuO9PS34031-32-83年 -20°C 粉末状
溶解性(25°C)
DMSO 10 mMWater <1 mMEthanol <1 mM
生物活性
Auranofin is an inhibitor of thioredoxin reductase (TrxR) (IC50 = 20 nM; Ki = 4 nM for the NADPH-reduced form of human cytosolic TrxR). Auranofin induced themitochondrial permeability transition via inhibition of mitochondrial TrxR. Auranofin also exhibits anti-inflammatory and immunosuppressive activities. Auranofininhibits 5-lipoxygenase at high concentrations and stimulates LTA hydrolase at low concentrations.
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠
重量 (kg)体表面积 (m2)Km 系数
0.020.0073
动物 B的Km系数动物 A的Km系数
大鼠0.150.0256
兔1.80.1512
豚鼠0.40.058
仓鼠0.080.025
狗100.520
动物 A (mg/kg) = 动物 B (mg/kg) ×
例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
参考文献
Auranofin blocks interleukin-6 signalling by inhibiting phosphorylation of JAK1 and STAT3. Kim NH, et al. Immunology. 2007 Dec;122(4):607-14. PMID: 17645497.
Induction of mitochondrial permeability transition by auranofin, a gold(I)-phosphine derivative. Rigobello MP, et al. Br J Pharmacol. 2002 Aug;136(8):1162-8. PMID: 12163349.
Human placenta thioredoxin reductase. Isolation of the selenoenzyme, steady state kinetics, and inhibition by therapeutic gold compounds. Gromer S, et al. J Biol Chem. 1998 Aug 7;273(32):20096-101. PMID: 9685351.
因篇幅问题不能全部显示,请点此查看更多更全内容