What is RU-58841?
RU-58841 (PSK-3841) is a non-steroidal antiandrogen compound originally developed by Roussel Uclaf (now Sanofi). It was designed for topical application to antagonize androgen receptor (AR) signaling locally in skin and hair follicle tissue without significant systemic antiandrogenic effects. RU-58841 competitively binds the androgen receptor, preventing dihydrotestosterone (DHT) and testosterone from activating AR-dependent gene transcription in target tissue. The compound was investigated in preclinical studies through Phase 1/2 clinical development for androgenetic alopecia before being discontinued, reportedly for commercial rather than safety reasons. RU-58841’s non-steroidal structure and rapid local metabolism were designed to limit systemic exposure and avoid the side effects associated with oral antiandrogens like finasteride or dutasteride. It remains a research compound studied in hair follicle and androgen biology contexts.
Mechanism of Action
RU-58841 has been investigated for its competitive antagonism of the androgen receptor in dermal papilla cells of hair follicles. DHT (dihydrotestosterone) normally binds the AR in these cells, triggering AR nuclear translocation, dimerization, and binding to androgen response elements (AREs) in gene promoters, inducing transcription of genes that shorten the anagen (growth) phase and promote follicular miniaturization. Researchers observed that RU-58841 competes with DHT for AR binding, preventing receptor activation and downstream gene expression changes associated with follicular regression. Studies suggest that topically applied RU-58841 is rapidly metabolized in skin tissue, limiting systemic absorption and circulating antiandrogen levels. In preclinical hair follicle models, researchers observed that RU-58841 treatment was associated with maintenance of hair follicle size and growth phase duration in androgen-sensitive follicles. The compound shows high AR binding affinity comparable to DHT but without agonist activity.
Published Research
Topical Antiandrogen Activity
Battmann et al. (1994) characterized RU-58841 as a topical antiandrogen with high androgen receptor affinity and rapid local metabolism, demonstrating its selective activity in skin tissue with limited systemic exposure [1].
Hair Follicle Biology
de Brouwer et al. (1997) investigated RU-58841 in the stumptail macaque model of androgenetic alopecia. Researchers observed that topical application was associated with reversal of follicular miniaturization and induction of hair regrowth in androgen-sensitive scalp regions [2].
Androgen Receptor Pharmacology
Teutsch et al. (1994) described the medicinal chemistry of RU-58841 and its non-steroidal AR antagonist scaffold, characterizing its binding kinetics and receptor selectivity profile [3].
Product Specifications
| Product | RU-58841 Lyophilized Powder |
|---|---|
| Available Sizes | 50mg x 30 ml, 50mg x 60 ml |
| Purity | ≥99% (HPLC verified) |
| CAS Number | 154992-24-2 |
| Molecular Formula | C₁₇H₁₈F₃N₃O₃ |
| Molecular Weight | 369.34 g/mol |
| Appearance | White lyophilized powder in glass vial |
| Storage | Store at -20°C desiccated. Protect from light and moisture. |
| Testing | Third-party tested — Certificate of Analysis available |
Frequently Asked Questions
RU-58841 is a non-steroidal antiandrogen compound designed for topical application. It competitively binds the androgen receptor to block DHT signaling in hair follicles.
The CAS registry number for RU-58841 is 154992-24-2.
No, RU-58841 is a non-steroidal small molecule. It is an androgen receptor antagonist, not a peptide.
Store RU-58841 at -20°C desiccated, protected from light and moisture.
Finasteride inhibits the enzyme 5u03b1-reductase that converts testosterone to DHT. RU-58841 blocks the androgen receptor directly, preventing DHT from binding. They act at different steps in the androgen pathway.
No, RU-58841 was studied through Phase 1/2 clinical development but was discontinued, reportedly for commercial reasons. It remains an investigational research compound.
References
- Battmann T, 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;48(1):55-60. PMID: 8136306
- de Brouwer B, et al. Biphasic response of pilosebaceous units to androgens in the stumptail macaque: topical application of RU 58841. J Invest Dermatol. 1997;109(4):495-499.
- Teutsch G, et al. Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor. J Steroid Biochem Mol Biol. 1994;48(1):111-119.
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