巴多昔芬-d4 是氘标记的巴多昔芬。 Bazedoxifene (TSE-424) 是一种口服的、可渗透 BBB 的非甾体选择性雌激素受体调节剂 (SERM)，对 ERα 和 ERβ 的 IC50 分别为 23 nM 和 99 nM。巴多昔芬可用于骨质疏松症的研究。 Bazedoxifene 还作为 IL-6/GP130 蛋白-蛋白相互作用的抑制剂，可用于胰腺癌的研究。
货号:ajcx21772
CAS:1133695-49-4
分子式:C30H30D4N2O3
分子量：474.6
溶解度:
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Bazedoxifene-d₄is intended for use as an internal standard for the quantification of bazedoxifene by GC- or LC-MS. Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC₅₀= 26 nM) and ERβ (IC₅₀= 99 nM).¹Bazedoxifene antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferationin vitroas well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).²It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.

1.Komm, B.S., Kharode, Y.P., Bodine, P.V.N., et al.Bazedoxifene acetate: A selective estrogen receptor modulator with improved selectivityEndocrinology146(9)3999-4008(2005) 2.Lewis-Wambi, J.S., Kim, H., Curpan, R., et al.The selective estrogen receptor modulator bazedoxifene inhibits hormone-independent breast cancer cell growth and down-regulates estrogen receptor α and cyclin D1Mol. Pharmacol.80(4)610-620(2011)