Raloxifene HCl

Modify Date: 2024-01-02 17:34:54

Raloxifene HCl structure	Common Name	Raloxifene HCl
	CAS Number	82640-04-8	Molecular Weight	510.044
	Density	1.285g/cm3	Boiling Point	728.2ºC at 760 mmHg
	Molecular Formula	C₂₈H₂₈ClNO₄S	Melting Point	143-147ºC
	MSDS	Chinese USA	Flash Point	394.2ºC

Use of Raloxifene HCl

Raloxifene hydrochloride(LY156758 hydrochloride) is a second generation selective estrogen receptor antagonist.Target: Estrogen receptorApproved: September 14, 2007Raloxifene activates TGF beta 3 promoter as a full agonist at nanomolar concentrations, and raloxifene inhibits the estrogen response element-containing vitellogenin promoter expression as a pure estrogen antagonist in transient transfection assays [1]. Raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with Ki values of 0.87 nM, 1.2 nM and 1.4 nM. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki of 51 nM [2]. Raloxifene (3 mg/kg/day) has potent estrogenic activity on bone resorption and serum cholesterol, a lesser effect on bone formation, and minimal activity on uterine wet weight in ovariectomized (OVX) rats. [3]. Raloxifene (0.1 mg/kg-10 mg/kg, orally for 5 weeks) increases bone mineral density in the distal femur and proximal tibia in ovariectomized (OVX) rat. Raloxifene reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat. Raloxifene diverges dramatically from estrogen in its lack of significant estrogenic effects on uterine tissue [4]. Raloxifene prevents cancellous osteopenia as well as the changes in radial bone growth, bone resorption, and blood cholesterol, but is less effective in reducing cancellous bone formation and does not prevent uterine atrophy in ovariectomized (OVX) rats [5].

Name	raloxifene hydrochloride
Synonym	More Synonyms

Description	Raloxifene hydrochloride(LY156758 hydrochloride) is a second generation selective estrogen receptor antagonist.Target: Estrogen receptorApproved: September 14, 2007Raloxifene activates TGF beta 3 promoter as a full agonist at nanomolar concentrations, and raloxifene inhibits the estrogen response element-containing vitellogenin promoter expression as a pure estrogen antagonist in transient transfection assays [1]. Raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with Ki values of 0.87 nM, 1.2 nM and 1.4 nM. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki of 51 nM [2]. Raloxifene (3 mg/kg/day) has potent estrogenic activity on bone resorption and serum cholesterol, a lesser effect on bone formation, and minimal activity on uterine wet weight in ovariectomized (OVX) rats. [3]. Raloxifene (0.1 mg/kg-10 mg/kg, orally for 5 weeks) increases bone mineral density in the distal femur and proximal tibia in ovariectomized (OVX) rat. Raloxifene reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat. Raloxifene diverges dramatically from estrogen in its lack of significant estrogenic effects on uterine tissue [4]. Raloxifene prevents cancellous osteopenia as well as the changes in radial bone growth, bone resorption, and blood cholesterol, but is less effective in reducing cancellous bone formation and does not prevent uterine atrophy in ovariectomized (OVX) rats [5].
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Endocrinology
References	[1]. Yang, N.N., et al., Estrogen and raloxifene stimulate transforming growth factor-beta 3 gene expression in rat bone: a potential mechanism for estrogen- or raloxifene-mediated bone maintenance. Endocrinology, 1996. 137(5): p. 2075-84. [2]. Obach, R.S., Potent inhibition of human liver aldehyde oxidase by raloxifene. Drug Metab Dispos, 2004. 32(1): p. 89-97. [3]. Sato, M., M.K. Rippy, and H.U. Bryant, Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. FASEB J, 1996. 10(8): p. 905-12. [4]. Black, L.J., et al., Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin Invest, 1994. 93(1): p. 63-9. [5]. Evans, G., et al., The effects of raloxifene on tibia histomorphometry in ovariectomized rats. Endocrinology, 1994. 134(5): p. 2283-8.

Description

Related Catalog

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Endocrinology

References

[1]. Yang, N.N., et al., Estrogen and raloxifene stimulate transforming growth factor-beta 3 gene expression in rat bone: a potential mechanism for estrogen- or raloxifene-mediated bone maintenance. Endocrinology, 1996. 137(5): p. 2075-84.

[2]. Obach, R.S., Potent inhibition of human liver aldehyde oxidase by raloxifene. Drug Metab Dispos, 2004. 32(1): p. 89-97.

[3]. Sato, M., M.K. Rippy, and H.U. Bryant, Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. FASEB J, 1996. 10(8): p. 905-12.

[4]. Black, L.J., et al., Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin Invest, 1994. 93(1): p. 63-9.

[5]. Evans, G., et al., The effects of raloxifene on tibia histomorphometry in ovariectomized rats. Endocrinology, 1994. 134(5): p. 2283-8.

Density	1.285g/cm3
Boiling Point	728.2ºC at 760 mmHg
Melting Point	143-147ºC
Molecular Formula	C₂₈H₂₈ClNO₄S
Molecular Weight	510.044
Flash Point	394.2ºC
Exact Mass	509.142761
PSA	98.24000
LogP	6.81510
Index of Refraction	1.654
Storage condition	-20°C Freezer
Water Solubility	DMSO: 28 mg/mL, soluble

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes	Xi
Risk Phrases	R36/37/38
Safety Phrases	22-24/25
RIDADR	NONH for all modes of transport
WGK Germany	3

Precursor 10
CAS#:84449-63-8 [4-(6-acetyloxy... CAS#:84449-80-9 4-[2-(1-Pipirid... CAS#:84541-36-6 Raloxifene Bism... CAS#:63675-74-1 6-Methoxy-2-(4-...
CAS#:84449-85-4 [6-[(methylsulf... CAS#:84449-90-1 Raloxifene CAS#:15570-12-4 4-Methoxythiophenol CAS#:166975-76-4 4-(2-PIPERIDINO...
CAS#:63675-73-0 4-Methoxy-alpha... CAS#:2632-13-5 PTP inhibitor 1
DownStream 1
CAS#:84449-90-1 Raloxifene

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[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone hydrochloride

[6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]{4-[2-(piperidin-1-yl)ethoxy]phenyl}methanone hydrochloride (1:1)

Raloxifene HCl

[6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanonhydrochlorid

1-[2-(4-{[6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]carbonyl}phenoxy)ethyl]piperidinium chloride

[6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]{4-[2-(1-piperidinyl)ethoxy]phenyl}methanone hydrochloride (1:1)

Methanone, [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-, hydrochloride (1:1)

methanone, [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-, hydrochloride

6-Hydroxy-2-(p-hydroxyphenyl)benzo(b)thien-3-yl-p-(2-piperidinoethoxy)phenyl ketone hydrochloride

MFCD01938233

Raloxifene hydrochloride

Raloxifene (hydrochloride)

DC Chemicals Limited
China
Product Name: Raloxifene HCl
Price: $300.0/1g
Purity: 98.0%
Stocking Period: 3 Day
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Zhejiang Hangyu API Co., Ltd
China
Product Name: Raloxifene hydrochloride Evista
Price: ￥Inquiry/1kg
Purity: 99.5%
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Henan Tianfu Chemical Co., Ltd.
China
Product Name: Raloxifene hydrochloride
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

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Raloxifene HCl

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