Methylstenbolone is a steroid and an anti-inflammatory agent. Methylstenbolone inhibits nitric oxide production in macrophages and exhibits cytotoxicity against breast cancer cells and normal fibroblasts. Methylstenbolone can be used for the research of inflammation and breast cancer [3].
In Vivo, Methylstenbolone (1 mg; i.g.; single dose) results in the production and urinary excretion of two dihydroxylated metabolites (U11 and U12) inchimeric and nonchimeric uPA+/+-SCID mice[1].
In Vitro, Methylstenbolone (1-25 μg/mL) potently inhibits nitric oxide production in J774.2 mouse macrophage cells with an IC50 of 10.1 μg/mL[3]. Methylstenbolone (6.25-50 µM; 48 h) is cytotoxic to MCF-7 human breast cancer cells (IC50 = 12.26 μg/mL) and toxic to BJ human fibroblast normal cells (IC50 = 8.69 μg/mL), but shows no cytotoxicity in NCI-H460 human lung cancer cells or HeLa human cervical cancer cells[3].
References:
[1]. Geldof L, et al. Metabolism of methylstenbolone studied with human liver microsomes and the uPA⁺/⁺-SCID chimeric mouse model. Biomed Chromatogr. 2014;28(7):974-985.
[2]. Piper T, et al. Studies on the in vivo metabolism of methylstenbolone and detection of novel long term metabolites for doping control analysis. Drug Test Anal. 2019;11(11-12):1644-1655.
[3]. Aamer M, et al. New anti-inflammatory and non-cytotoxic metabolites of methylstenbolone obtained by microbial transformation. Bioorg Chem. 2022;129:106187.
In Vivo, Methylstenbolone (1 mg; i.g.; single dose) results in the production and urinary excretion of two dihydroxylated metabolites (U11 and U12) inchimeric and nonchimeric uPA+/+-SCID mice[1].
In Vitro, Methylstenbolone (1-25 μg/mL) potently inhibits nitric oxide production in J774.2 mouse macrophage cells with an IC50 of 10.1 μg/mL[3]. Methylstenbolone (6.25-50 µM; 48 h) is cytotoxic to MCF-7 human breast cancer cells (IC50 = 12.26 μg/mL) and toxic to BJ human fibroblast normal cells (IC50 = 8.69 μg/mL), but shows no cytotoxicity in NCI-H460 human lung cancer cells or HeLa human cervical cancer cells[3].
References:
[1]. Geldof L, et al. Metabolism of methylstenbolone studied with human liver microsomes and the uPA⁺/⁺-SCID chimeric mouse model. Biomed Chromatogr. 2014;28(7):974-985.
[2]. Piper T, et al. Studies on the in vivo metabolism of methylstenbolone and detection of novel long term metabolites for doping control analysis. Drug Test Anal. 2019;11(11-12):1644-1655.
[3]. Aamer M, et al. New anti-inflammatory and non-cytotoxic metabolites of methylstenbolone obtained by microbial transformation. Bioorg Chem. 2022;129:106187.