Y134

Y134 is a selective estrogen receptor modulator (SERM) and derivative of raloxifene (Item No. 10011620).¹ It selectively binds to estrogen receptor α (ERα) over ERβ (K_is = 0.09 and 11.31 nM, respectively) and does not bind to the androgen, progesterone, glucocorticoid, or mineralocorticoid receptors. Y134 also selectively inhibits estradiol-induced activation of ERα over ERβ in reporter assays using CV-1 cells (IC₅₀s = 0.52 and 2.94 nM, respectively). Y134 (1 µM) binds to cannabinoid 1 (CB₁) and CB₂ receptors in CHO cells expressing the human receptors and reduces basal activity in the same cells when used at a concentration of 10 µM.² It also activates the aryl hydrocarbon receptor (AhR) in a reporter assay using Hepa1 cells when used at a concentration of 10 µM.³ Y134 inhibits estradiol-induced proliferation of MCF-7 and T47D breast cancer cells (IC₅₀s = 3.95 and 41.1 nM, respectively).¹ In vivo, Y134 increases bone mineral density and uterine weight in ovariectomized mice.⁴

WARNING This product is not for human or veterinary use.

1. Ning, M., Zhou, C., Weng, J., et al. Biological activities of a novel selective oestrogen receptor modulator derived from raloxifene (Y134). Br. J. Pharmacol. 150(1), 19-28 (2007).

2. Franks, L.N., Ford, B.M., and Prather, P.L. Selective estrogen receptor modulators: Cannabinoid receptor inverse agonists with differential CB₁ and CB₂ selectivity. Front. Pharmacol. 7, 503 (2016).

3. Jang, H.S., Pearce, M., O'Donnell, E.F., et al. Identification of a raloxifene analog that promotes AhR-mediated apoptosis in cancer cells. Biology (Basel) 6(4), 41 (2017).

4. Yang, C., Xu, G., Li, J., et al. Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor α and their bioactivities in vivo. Bioorg. Med. Chem. Lett. 15(5), 1505-1507 (2005).