| Identification | Back Directory | [Name]
Carbamic acid, N-[(4aR,4bS,6aS,7S,9aS,9bS,11aR)-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1,4a,6a-trimethyl-2-oxo-1H-indeno[5,4-f]quinolin-7-yl]-, 2,2,2-trifluoroethyl ester | [CAS]
796885-38-6 | [Synonyms]
MK-4541
Carbamic acid, N-[(4aR,4bS,6aS,7S,9aS,9bS,11aR)-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1,4a,6a-trimethyl-2-oxo-1H-indeno[5,4-f]quinolin-7-yl]-, 2,2,2-trifluoroethyl ester | [EINECS(EC#)]
692-949-8 | [Molecular Formula]
C22H31F3N2O3 | [MOL File]
796885-38-6.mol | [Molecular Weight]
428.49 |
| Hazard Information | Back Directory | [Description]
MK-4541 is a Selective Androgen Receptor Modulator (SARM). | [Uses]
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model[1]. | [in vivo]
MK-4541 (100 mg/kg; p.o.; 5 times per week for 5 weeks) inhibits prostate tumor growth in athymic nude mice bearing R-3327-G cells[1].
MK-4541 (100 mg/kg, 200 mg/kg; p.o.; 5 times per week for 5 weeks) exhibits anti-androgen effects on the seminal vesicles, reduces plasma testosterone concentrations in intact males, and inhibits Ki67 expression[1].
MK-4541 (15 mg/kg, 50 mg/kg; p.o.; 5 times per week for 8 weeks) causes the loss of musculoskeletal mass and function in adult castrated mice[1].
| Animal Model: | R3327-G prostate tumors in xenograft mouse model[1] | | Dosage: | 25 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg | | Administration: | Oral gavage; once daily, 5 times per week for 5 weeks | | Result: | Significantly inhibited tumor growth at 100 mg/kg, as well as reducing plasma testosterone concentration and Ki67 expression. |
| [References]
[1] Chisamore MJ, et al. A novel selective androgen receptor modulator (SARM) MK-4541 exerts anti-androgenic activity in the prostate cancer xenograft R-3327G and anabolic activity on skeletal muscle mass & function in castrated mice. J Steroid Biochem Mol Biol. 2016 Oct;163:88-97. DOI:10.1016/j.jsbmb.2016.04.007 |
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