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CAS No.: 154992-24-2

RU 58841 Catalog No. CSN12743

Synonyms: PSK-3841;HMR-3841

RU 58841 is a nonsteroidal antiandrogen for potential use as a topical treatment for androgen-dependent conditions including acne, pattern hair loss, and excessive hair growth.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述The androgen receptor (AR) and the androgen-AR signaling pathway play a significant role in male sexual differentiation and the development and function of male reproductive and non-reproductive organs ^[3]. RU 58841, a new topically active nonsteroidal anti-androgen, displays a high binding affinity for the AR (k_a=1.1 nM). And the IC₅₀ value for RU 58841 was 100 nM. PC3 cells were cotransfected with a wt AR expression plasmid, and incubated with both 1 nM DHT and a series of concentrations of RU 58841. RU 58841 suppressed DHT's effects in PC3 cells with the wt AR in a dose-dependent manner, indicating that this compound exerts antagonistic effects. 5% RU 58841 was applied on the bald scalp of the stumptailed macaques. The folliculogram analysis revealed that all four treated cases showed a marked progressive pattern of folliculograms in 5 mo. Moreover, when topically applied, RU 58841 exerted apotent dose-dependent regression of the hamster flank organ. Likewise, topical RU 58841 induced remarkable effects on hair and follicular regrowth in the bald frontal scalp of macaques, which indicated that topical RU 58841 was a clinically hopeful therapy for androgenetic alopecia ^[4].
动物研究
剂量
Rat^[2]: 0.3 mg/rat (percutaneous); 1 mg/rat (s.c.); 10 mg/rat (p.o.)

给药途径
percutaneous, s.c., p.o.
参考文献

动物研究
剂量	Rat^[2]: 0.3 mg/rat (percutaneous); 1 mg/rat (s.c.); 10 mg/rat (p.o.)
给药途径	percutaneous, s.c., p.o.

[1] Munster U, Nakamura C, et al. RU 58841-myristate--prodrug development for topical treatment of acne and androgenetic alopecia. Pharmazie. 2005 Jan;60(1):8-12.
[2] Battmann T, Bonfils A, et al. RU 58841, a new specific topical antiandrogen: a candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism. J Steroid Biochem Mol Biol. 1994 Jan;48(1):55-60.
[3] Shukla GC, Plaga AR, Shankar E, Gupta S. Androgen receptor-related diseases: what do we know? Andrology. 2016 May;4(3):366-81. doi: 10.1111/andr.12167. Epub 2016 Mar 16. PMID: 26991422.
[4] Pan HJ, Wilding G, Uno H, Inui S, Goldsmith L, Messing E, Chang C. Evaluation of RU58841 as an anti-androgen in prostate PC3 cells and a topical anti-alopecia agent in the bald scalp of stumptailed macaques. Endocrine. 1998 Aug;9(1):39-43. doi: 10.1385/ENDO:9:1:39. PMID: 9798729.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7075 mL
- 13.5377 mL
- 27.0754 mL
- 5 mM
- 0.5415 mL
- 2.7075 mL
- 5.4151 mL
- 10 mM
- 0.2708 mL
- 1.3538 mL
- 2.7075 mL

技术信息

CAS号

154992-24-2

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H18F3N3O3

运输

蓝冰

分子量

369.34

别名

PSK-3841;HMR-3841

溶解度

DMSO	73.0 mg/mL (197.7 mM)
Water	Insoluble
Ethanol	73.0 mg/mL (197.7 mM)

动物实验配方

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