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Evista(Raloxifene HCl)

Raloxifene is estrogen antagonists, inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.

Catalog No.S1227

: Tel: +1-832-582-8158[email protected]

Evista(Raloxifene HCl) Chemical Structure
Molecular Weight: 510.04

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Evista(Raloxifene HCl) is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) FDA Approved Drug Library (96-well)

Product Information

Compare Estrogen/progestogen Receptor Chemicals

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Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1191	Fulvestrant (Faslodex)	<1 mg/mL	121 mg/mL	121 mg/mL
S1972	Tamoxifen Citrate (Nolvadex)	<1 mg/mL	113 mg/mL	<1 mg/mL
S1227	Evista(Raloxifene HCl)	<1 mg/mL	102 mg/mL	<1 mg/mL
S1776	Toremifene Citrate (Fareston, Acapodene)	<1 mg/mL	120 mg/mL	<1 mg/mL
S2606	Mifepristone (Mifeprex)	<1 mg/mL	86 mg/mL	19 mg/mL
S1251	Dienogest	<1 mg/mL	62 mg/mL	5 mg/mL
S1598	LY500307 (Erteberel)	<1 mg/mL	57 mg/mL	57 mg/mL
S1377	Drospirenone	<1 mg/mL	73 mg/mL	11 mg/mL
S1376	Gestodene	<1 mg/mL	62 mg/mL	8 mg/mL
S1665	Estrone	<1 mg/mL	54 mg/mL	<1 mg/mL
S2466	Estriol	<1 mg/mL	57 mg/mL	10 mg/mL
S2473	Hexestrol(Bibenzyl)	<1 mg/mL	42 mg/mL	42 mg/mL
S2450	Equol	<1 mg/mL	48 mg/mL	48 mg/mL
S2561	Clomifene citrate (Serophene)	<1 mg/mL	120 mg/mL	11 mg/mL
S2567	Medroxyprogesterone acetate	<1 mg/mL	12 mg/mL	12 mg/mL
S2611	Ethisterone	<1 mg/mL	0.05 mg/mL	<1 mg/mL
S1914	Pregnenolone	<1 mg/mL	22 mg/mL	22 mg/mL
S2832	Epiandrosterone (3β-androsterone)	<1 mg/mL	58 mg/mL	58 mg/mL
S3167	Altrenogest	<1 mg/mL	62 mg/mL	2 mg/mL
S3149	Estradiol valerate	<1 mg/mL	71 mg/mL	<1 mg/mL
S3160	Ethynodiol diacetate	77 mg/mL	77 mg/mL	<1 mg/mL
S2128	Bazedoxifene HCl	<1 mg/mL	101 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	Raloxifene is estrogen antagonists, inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.
Targets	Estrogen
IC50	5.7 nM ^[1]
In vitro	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. ^[1] Raloxifene 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. ^[2]
In vivo	Raloxifene restores both bone mineral density and TGF beta 3 messenger RNA expression in the femur to levels measured in intact rats. ^[2] 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. ^[3] 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. ^[4] 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. ^[5]
Clinical Trials	Raloxifene is in phase 4 clinical trial in patients with osteoporosis.
Features	Raloxifene is as effective as tamoxifen in reducing the incidence of breast cancer in postmenopausal women at increased risk.

Protocol(Only for Reference)

Kinase Assay: ^[1]

Phthalazine Oxidase Assay	Phthalazine is incubated with human liver cytosol (0.05 mg/mL) in a total volume of 0.2 mL of 25 mM KH₂PO4, pH 7.4, containing 0.1 mM EDTA, in the presence and absence of Raloxifene. Raloxifene is added in dimethyl sulfoxide such that the final concentration of solvent is 1% (v/v). Incubations are conducted open to the air for 2.5 min in a water bath set at 37℃. Initial time course experiments establish the linearity of reaction velocity versus protein concentration and incubation time. In preincubation experiments, Raloxifene is incubated with cytosol for 30 min at 37℃ before addition of phthalazine. The incubations are terminated by the addition of 0.05 mL of formic acid (1 M) containing 4-methyl-1-phthalazinone (25 ng) as an internal standard. Terminated incubation mixtures are subjected to filtration through a 0.45-μm mixed cellulose ester 96-well membrane vacuum filtration module into 96-well plates.

Phthalazine Oxidase Assay

Phthalazine is incubated with human liver cytosol (0.05 mg/mL) in a total volume of 0.2 mL of 25 mM KH₂PO4, pH 7.4, containing 0.1 mM EDTA, in the presence and absence of Raloxifene. Raloxifene is added in dimethyl sulfoxide such that the final concentration of solvent is 1% (v/v). Incubations are conducted open to the air for 2.5 min in a water bath set at 37℃. Initial time course experiments establish the linearity of reaction velocity versus protein concentration and incubation time. In preincubation experiments, Raloxifene is incubated with cytosol for 30 min at 37℃ before addition of phthalazine. The incubations are terminated by the addition of 0.05 mL of formic acid (1 M) containing 4-methyl-1-phthalazinone (25 ng) as an internal standard. Terminated incubation mixtures are subjected to filtration through a 0.45-μm mixed cellulose ester 96-well membrane vacuum filtration module into 96-well plates.

Animal Study: ^[3]

Animal Models	ovariectomized (OVX) rat
Formulation	1.5% carboxymethylcellulose
Dosages	10 mg/kg
Administration	Orally

References

Chemical Information

Download Evista(Raloxifene HCl) SDF

Molecular Weight (MW)	510.04
Formula	C₂₈H₂₇NO₄S.HCl
CAS No.	82640-04-8
Synonyms	Raloxifene Hydrochloride, keoxifene

Solubility (25°C) DMSO 102 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name

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Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Evista(Raloxifene HCl)