Bazedoxifene-d4 |
| カタログ番号GC46907 |
バゼドキシフェン-d4 は、重水素標識バゼドキシフェンです。バゼドキシフェン (TSE-424) は経口の BBB 浸透性非ステロイド性選択的エストロゲン受容体モジュレーター (SERM) で、ERα と ERβ の IC50 はそれぞれ 23 nM と 99 nM です。バゼドキシフェンは、骨粗鬆症の研究に使用できます。バゼドキシフェンは、IL-6/GP130 タンパク質間相互作用の阻害剤としても作用し、膵臓がんの研究に使用できます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1133695-49-4
Sample solution is provided at 25 µL, 10mM.
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Bazedoxifene-d4 is 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).1 Bazedoxifene antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).2 It 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)
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