Bazedoxifene-d4 |
| Katalog-Nr.GC46907 |
Bazedoxifen-d4 ist Deuterium-markiertes Bazedoxifen. Bazedoxifen (TSE-424) ist ein oraler, BBB-penetranter nichtsteroidaler selektiver Östrogenrezeptormodulator (SERM) mit IC50-Werten von 23 nM und 99 nM fÜr ERα bzw. ERβ. Bazedoxifen kann zur Erforschung von Osteoporose eingesetzt werden. Bazedoxifen wirkt auch als Inhibitor von IL-6/GP130-Protein-Protein-Wechselwirkungen und kann fÜr die Erforschung von BauchspeicheldrÜsenkrebs verwendet werden.
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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