Bazedoxifene-d4 |
Catalog No.GC46907 |
Le bazédoxifène-d4 est un bazédoxifène marqué au deutérium. Le bazédoxifène (TSE-424) est un modulateur sélectif non stéroÏdien des récepteurs aux œstrogènes (SERM) pénétrant dans la BBB, avec des IC50 de 23 nM et 99 nM pour ERα et ERβ, respectivement. Le bazédoxifène peut être utilisé pour la recherche de l'ostéoporose. Le bazédoxifène agit également comme un inhibiteur des interactions protéine-protéine IL-6/GP130 et peut être utilisé pour la recherche sur le cancer du pancréas.
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.
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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