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Bazedoxifene

Names

[ CAS No. ]:
198481-32-2

[ Name ]:
Bazedoxifene

[Synonym ]:
TSE-424
Bazedoxifene
1H-Indol-5-ol, 1-[[4-[2-(hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-
1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-indol-5-ol
1-{4-[2-(Azepan-1-yl)ethoxy]benzyl}-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol
Bazedoxifeno
1-{4-[2-(1-Azepanyl)ethoxy]benzyl}-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-
Conbriza

Biological Activity

[Description]:

Bazedoxifene is a selective estrogen receptor modulator (SERM) currently in development for osteoporosis prevention and treatment.IC50 value:Target: estrogen receptor modulatorPreclinical and clinical studies with bazedoxifene demonstrate more tissue selectivity than other SERMs. In particular, bazedoxifene has minimal if any agonist activity in the uterus and is able to antagonize effects of estrogen on the uterus. Animal studies and early clinical studies suggest effects in the bone similar to other SERMs with prevention of postmenopausal bone loss.

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR
Research Areas >> Cancer

[References]

[1]. Lewis-Wambi JS, et al. The selective estrogen receptor modulator bazedoxifene inhibits hormone-independent breast cancer cell growth and down-regulates estrogen receptor α and cyclin D1. Mol Pharmacol. 2011 Oct;80(4):610-20.

[2]. Duggan ST, McKeage K. Bazedoxifene: a review of its use in the treatment of postmenopausal osteoporosis. Drugs. 2011 Nov 12;71(16):2193-212.

[3]. Lello S, Brandi ML, Minisola G et al. Bazedoxifene: literature data and clinical evidence. Clin Cases Miner Bone Metab. 2011 Sep;8(3):29-32.

[4]. Komm BS, Chines AA. Bazedoxifene: the evolving role of third-generation selective estrogen-receptor modulators in the management of postmenopausal osteoporosis. Ther Adv Musculoskelet Dis. 2012 Feb;4(1):21-34.


[Related Small Molecules]

Elacestrant dihydrochloride | AZD9496 | Kaempferol | XCT 790 | Estrone | GDC-0810 | (20S)-Protopanaxatriol | 27-Hydroxycholesterol | Diethylstilbestrol | PHTPP | 2,3-bis(4-hydroxyphenyl)propionitrile | 4',7-Isoflavandiol | cholesterol | Chrysin | Endoxifen (Z-isomer hydrochloride)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
694.4±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C30H34N2O3

[ Molecular Weight ]:
470.603

[ Flash Point ]:
373.8±31.5 °C

[ Exact Mass ]:
470.256958

[ PSA ]:
57.86000

[ LogP ]:
6.59

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.622

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds