Bazedoxifene Struktur

Bazedoxifene

Bezeichnung:Bazedoxifene

CAS-Nr198481-32-2

Englisch Name:Bazedoxifene

CBNumberCB01458163

SummenformelC30H34N2O3

Molgewicht470.6

MOL-Datei198481-32-2.mol

Bazedoxifene physikalisch-chemischer Eigenschaften

Schmelzpunkt	98-102°
Siedepunkt	694.4±55.0 °C(Predicted)
Dichte	1.19
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
pka	10.12±0.15(Predicted)
Farbe	White to Very Dark Beige

Gefahreninformationscode (GHS)

Bazedoxifene Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Bazedoxifene is an nonsteroidal selective estrogen receptor modulator (SERM). Bazedoxifene is used as an antiosteoporotic.
Definition
ChEBI: Bazedoxifene is a phenylindole.
Allgemeine Beschreibung
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.
Enzyminhibitor
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 Upstream-Materialien And Downstream Produkte

Bazedoxifene Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

198481-32-2, Bazedoxifene Verwandte Suche:

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