Chemical raw material peptide anti hair loss RU58841 / RU 58841 / 154992-24-2

Chemical raw material peptide anti hair loss RU58841 / RU 58841 / 154992-24-2

Product Name: RU-58841

Molecular Formula: C17H18F3N3O3

Molecular Weight : 369.3

Cas No. : 154992-24-2

Appearance: White Powder

Specification: 99%

Packing :100g/bag or according to Customer request

Description : RU-58841 (also known as PSK-3841 or HMR-3841) is a non-steroidal antiandrogen which was previously investigated for use as a topical treatment for acne, androgenetic alopecia, and hirsutism.

RU-58841 is an androgen receptor (AR) inhibitor capable of blocking 70% of DHT binding. When compared with the antiandrogenic compound cyproterone acetate, RU-58841 exhibited a 20% increase in AR binding. This compound binds to both the ligand and regulatory domains of the androgen receptor. RU-58841 exerts allosteric binding effects. The effect of androgen receptor transcriptional activation by RU58841, a nonsteroidal anti-androgen, was studied in the human prostate cancer PC3 cell line by cotransfection with wild-type androgen receptor (wt AR) and an androgen-responsive reporter (MMTV-ARE-CAT) construct. Anti-and rogens, hydroxyflutamide, and Casodex, and the antiestrogen, genistein, were studied in parallel for comparison with RU58841. The wt AR was activated only by the androgen dihydrotestosterone (DHT). Neither the anti-androgens nor antiestrogen can enhance AR transcriptional activity at 10(-11)-10(-7)M in PC3 cells. Hydroxyflutamide, RU58841, and Casodex, but not genistein, displayed competitively suppressive effects on DHT activation of wt AR. The potency of RU58841 was comparable to that of hydroxyflutamide.

RU58841, on topical application, revealed a potent increase in density, thickening, and length of hair in the macaque model of androgenetic alopecia, whereas no systemic effects were detected. Using the macaque model of androgenetic alopecia,the effects of two antiandrogens, oral finasteride (FS) and topical RU58841 (RU), were examined on follicular regrowth and serum levels of T and DHT. FS is known to inhibit type II reductase and to induce follicular growth in the macaque bald scalp (Rhodes et al., J.C.E.M. 79:991, 1994). RU, a potent non-steroidal androgen receptor (AR) blocker, reduces the size of hamster flank organs by topical application (Battmann et al., J. Steroid. Biochem. Molec. Biol. 48:55, 1944). FS (1mg/kg/day) and placebo, in 10 animals each, were given for 6 months. RU (5, 0.5%) and vehicle (0.5ml/kg/day) were topically applied in a total of 10 animals (4,3,3). Skin biopsies for micromorphometric analysis (folliculogram) were taken at 0 and 6 months for FS and at 0 and 4 months for RU. The populations of anagen follicles and vellus follicles enlarged to terminal size were compared to those in pre-treatment stages; anagen follicles increased an average of 88% with FS and 103% with RU (5%) and growth of vellus follicles to terminal size was 12% with FS, and 26% with RU (5%). RU (0.5%) showed a weak effect and placebos induced no effect. Hair regrowth was observed in varying degrees with both agents; RU (5%) induced the most growth after only 2 months of treatment for hair loss. Plasma RU and metabolites (10-20 ng/ml) were detected in 2 cases (5%) at 3, and one at 6, months. Serum DHT decreased about 70% and T (males) increased with FS, but exhibited no significant changes with RU.

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