| Identification | Back Directory | [Name]
Bazedoxifene | [CAS]
198481-32-2 | [Synonyms]
CS-1993
Tse-424
Batoxifene
Bazedoxifen
Bazedoxifene
Bazedoxifeno
Unii-Q16tt9C5bk
BAZEDOXIFENE BASE
Bazedoxifene [inn]
Bazedoxifene free base
Bazedoxifeno [inn-spanish]
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- | [EINECS(EC#)]
805-732-1 | [Molecular Formula]
C30H34N2O3 | [MDL Number]
MFCD05148441 | [MOL File]
198481-32-2.mol | [Molecular Weight]
470.6 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C |
|
|