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Enobosarm-d4 is intended for use as an internal standard for the quantification of enobosarm by GC- or LC-MS. Enobosarm is a non-steroidal selective androgen receptor modulator (SARM; Ki = 0.0038 µM in a radioligand binding assay).1 It is a partial agonist of the androgen receptor (IC50 = 0.0364 µM in a transactivation assay) and inhibits the proliferation of 22Rv1, DU145, LNCaP, and VCaP prostate cancer cells (IC50s = 24.77, 44.55, 20.9, and 24.47 µM, respectively).2 Enobosarm (0.001 and 0.01 µM) inhibits lipogenesis in isolated rat adipocytes.3 It increases the weights of the prostate gland and seminal vesicles, markers of androgenic activity, and the levator ani muscle, a marker of anabolic activity, in castrated rats (ED50s = 0.12, 0.39, and 0.03 mg/day, respectively).1

1.Kim, J., Wu, D., Hwang, D.J., et al.The para substituent of S-3-(phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamides is a major structural determinant of in vivo disposition and activity of selective androgen receptor modulatorsJ. Pharmacol. Exp. Ther.315(1)230-239(2005) 2.Bassetto, M., Ferla, S., Pertusati, F., et al.Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancerEur. J. Med. Chem.118230-243(2016) 3.Leciejewska, N., Pruszynska-Oszmalek, E., Bien, J., et al.Effect of ostarine (enobosarm/GTX024), a selective androgen receptor modulator, on adipocyte metabolism in Wistar ratsJ. Physiol. Pharmacol.70(4)525-533(2019)

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