RU 58841

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Chemical Structure| 154992-24-2 同义名 : HMR-3841; PSK-3841
CAS号 : 154992-24-2
货号 : A108339
分子式 : C17H18F3N3O3
纯度 : 99%
分子量 : 369.34
MDL号 : MFCD00925776
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
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 (ka=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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.54mL

2.71mL

1.35mL

27.08mL

5.42mL

2.71mL

参考文献

[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.