Bazedoxifene Chemical 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

Bazedoxifene Usage And Synthesis

Uses

Bazedoxifene is an nonsteroidal selective estrogen receptor modulator (SERM). Bazedoxifene is used as an antiosteoporotic.

Definition

ChEBI: Bazedoxifene is a phenylindole.

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.

target

estrogen receptor

Bazedoxifene(198481-32-2)Related Product Information

• FLAVOXATE
• Olaparib
• Indacaterol
• CETUXIMAB
• Baclofen
• VILAZODONE
• Rivaroxaban
• Liraglutide
• Capecitabine
• Sofosbuvir
• Dapoxetine
• 1-[[4-[2-(Hexahydro-1-oxido-1H-azepin-1-yl)ethoxy]phenyl]Methyl]-2-(4-hydroxyphenyl)-3-Methyl-1H-indol-5-ol
• BAZEDOXIFENE ACETATE
• 4-[2-(DIMETHYLAMINO)ETHOXY]BENZYLAMINE
• 1-Ethyl-2-phenylindole
• Bazedoxifene
• 1-[4-(2-AZEPAN-1-YL-ETHOXY)-BENZYL]-5-BENZYLOXY-2-(4-BENZYLOXY-PHENYL)-3-METHYL-1H-INDOLE
• 1,3-DIMETHYL-2-PHENYLINDOLE