Bazedoxifene

Bazedoxifene Structure
CAS No.
198481-32-2
Chemical Name:
Bazedoxifene
Synonyms
Tse-424;CS-1993;Batoxifene;Bazedoxifen;Bazedoxifene;Bazedoxifeno;Unii-Q16tt9C5bk;BAZEDOXIFENE BASE;Bazedoxifene [inn];Bazedoxifene free base
CBNumber:
CB01458163
Molecular Formula:
C30H34N2O3
Molecular Weight:
470.6
MOL File:
198481-32-2.mol
MSDS File:
SDS
Modify Date:
2023/10/31 12:04:19

Bazedoxifene Properties

Melting point 98-102°
Boiling point 694.4±55.0 °C(Predicted)
Density 1.19
storage temp. Sealed in dry,Store in freezer, under -20°C
solubility Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
form Solid
pka 10.12±0.15(Predicted)
color White to Very Dark Beige

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS08
Signal word  Danger
Hazard statements  H360
Precautionary statements  P201-P202-P281-P308+P313-P405-P501

Bazedoxifene Chemical Properties,Uses,Production

General Description

Bazedoxifene, 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol (Viviant), was declared to be “approvable” bythe FDA in 2007 for the prevention of postmenopausalosteoporosis. As of mid-2009, final approval in the UnitedStates is still pending. Bazedoxifene was approved inEurope in 2009 for the treatment of post–menopausalosteoporosis.

Clinical Use

Bazedoxifene is an indole-based SERM that is under investigation for the treatment and prevention of postmenopausal osteoporosis. It also is being evaluated in combination with Premarin (conjugated estrogens). Bazedoxifene displaces 17β-estradiol from estrogen receptors and has excellent binding affinity for the receptor itself. Unlike raloxifene, this agent does not cause hot flashes at the doses required to have a beneficial effect on bone. In addition, it does not cause uterine or mammary gland stimulation.

Enzyme inhibitor

This potent and selective estrogen receptor modulator, or SERM (FW = 530.65 g/mol; CAS 198481-33-3; Solubility: 00 mM in DMSO), also named 1-[[4-[2- (hexahydro-1H-azepin-1-yl) ethoxy]phenyl]methyl]-2- (4- hydroxyphenyl) -3-methyl-1H-indol-5-ol, selectivity targets the extrogen receptor ERα (IC50 = 26 nM), with weaker action against ERβ (IC50 = 99 nM), inhibiting 17β-estradiol-induced proliferation of MCF-7 cells. Bazedoxifene represents a promising new treatment for osteoporosis, one with a potential for less uterine and vasomotor effects than selective estrogen receptor modulators now used clinically.

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1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-indol-5-ol 1-((4-(2-Hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol 1H-Indol-5-ol, 1-((4-(2-(hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl- Bazedoxifene Bazedoxifene [inn] Bazedoxifeno Bazedoxifeno [inn-spanish] Tse-424 Unii-Q16tt9C5bk Bazedoxifen CS-1993 Batoxifene BAZEDOXIFENE BASE Bazedoxifene free base 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphen... 1-(4-(2-(Azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol 198481-32-2 C30H34N2O3 Aromatics Heterocycles Intermediates & Fine Chemicals Pharmaceuticals