Bazedoxifene

Modify Date: 2024-01-03 01:16:02

Bazedoxifene Structure
Bazedoxifene structure
Common Name Bazedoxifene
CAS Number 198481-32-2 Molecular Weight 470.603
Density 1.2±0.1 g/cm3 Boiling Point 694.4±55.0 °C at 760 mmHg
Molecular Formula C30H34N2O3 Melting Point N/A
MSDS N/A Flash Point 373.8±31.5 °C

 Use of Bazedoxifene


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.

 Names

Name 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol
Synonym More Synonyms

 Bazedoxifene 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
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.

 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

 Synonyms

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
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