RU 58841_Androgen Receptor_CAS号154992-24-2说明书_AbMole中国

化学数据

分子量分子式CAS号储存条件

369.34

C17H18F3N3O3154992-24-23年 -20°C 粉末状

溶解性（25°C）

DMSO 10 mMWater <1 mMEthanol <1 mM

生物活性

RU 58841 is a specific androgen receptor antagonist or anti-androgen used as a topical treatment for acne, androgenetic alopecia and hirsutism. RU 58841displays high affinity for the hamster prostate and flank organ (F.O.) androgen receptors. In vivo, when topically applied, it exerts a potent dose-dependentregression of F.O. area at a dose as low as 1 microgram/animal while being devoid of antiandrogenic activity on deep accessory sex organs and of any effect ontestosterone level up to 100 micrograms/animal. RU 58841 has a dramatic effect on hair regrowth.

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

RU 58841, a new specific topical antiandrogen: a candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism. Battmann T, et al. J Steroid Biochem Mol Biol. 1994 Jan;48(1):55-60. PMID: 8136306.