RU 58841 is a specific androgen receptor antagonist or anti-androgen used as a topical treatment for acne, androgenetic alopecia and hirsutism. RU 58841 displays high affinity for the hamster prostate and flank organ (F.O.) androgen receptors. In vivo, when topically applied, it exerts a potent dose-dependent regression 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 on testosterone level up to 100 micrograms/animal. RU 58841 has a dramatic effect on hair regrowth.
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Source | Proc Natl Acad Sci U S A (2008). Figure 4. RU58841 |
| Method | Western immunoblot analysis | |
| Cell Lines | Human prostate cancer DU145 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 30 min | |
| Results | In contrast, genistein, RU486, and RU58841 had only marginal agonist activity (within 4-fold). |
| Molecular Weight | 369.34 |
| Formula | C17H18F3N3O3 |
| CAS Number | 154992-24-2 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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