Bazedoxifene acetate

Synonym
Product Category
Product Code
CAS Number
MDL Number
Pubchem CID
Reaxys RN
TSE-424, WAY-140424, WAY-TSE-424
API & Intermediates
KAPI0F05
198481-33-3
MFCD09260074
154256
10510865
image-155171-Trimethyl(trifluoromethyl)silane_reagent.png
Chemical Name
Molecular Formula
Molecular Weight
Assay
Appearance
Melting Point
Packaging
Storage
Bazedoxifene acetate
C32H38N2O5
530.66
≥98%(HPLC)
White to Beige Solid
178-179°C
10g,20g,50g,100g,500g,1kg and 5kg
-20°C Freezer (shipped in wet ice)
Bazedoxifene acetate (1-[4-(2-Azepan-1-yl-ethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetate) is a third generation nonsteroidal selective estrogen receptor modulator (SERM), used clinically to treat postmenopausal osteoporosis and also being studied for possible treatment of breast cancer and pancreatic cancer. Bazedoxifene binds to estrogen receptor-α with IC50 = 26 nM, similar to that of raloxifene, but lower affinity than 17-β estradiol. Bazedoxifene did not stimulate proliferation of MCF-7 cells, instead inhibited 17β -estradiol-induced proliferation with IC50 = 0.19 nM, exhibiting a desirable profile of agonist/antagonist activity.
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. [1]
In vitro metabolism, permeability, and efflux of bazedoxifene in humans. [2]
Relaxant Effects of the Selective Estrogen Receptor Modulator, Bazedoxifene, and Estrogen Receptor Agonists in Isolated Rabbit Basilar Artery. [3]
The Tissue-Selective Estrogen Complex (Bazedoxifene/Conjugated Estrogens) for the Treatment of Menopause. [4]
Effects of Bazedoxifene on Bone Mineral Density and Fracture in Post-Menopausal Osteoporotic Women: a Systematic Review and Meta-Analysis. [5]
References:
[1] C.P.Miller, et al, J. Med. Chem., 2001, 44(11), pp 1654-1657.
[2] L.Shen, et al, Drug Metab. Dispos., 2010, 38(9), pp 1471-1479.
[3] M.Castello-Ruiz, et al, J. Cardiovasc. Pharmacol., 2016, 68(4), pp 313-321.
[4] S.Lello, et al, Int. J. Endocrinol., 2017, art. no. 5064725.
[5] M.Khalili, et al, Clin. Rev. Bone Miner. Metab., 2018, 16(1), pp 22-32.
Signal Word
Hazard Statements
Precautionary Statements
HS Code
RIDADR
Legal Information
Not a hazardous substance or mixture


2933998090
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