
Raloxifene hydrochloride
CAS No. 82640-04-8
Raloxifene hydrochloride( Keoxifene | LY156758 )
Catalog No. M16068 CAS No. 82640-04-8
RaloxifeneHcl(LY156758 Hcl) is a second generation selective estrogen receptor antagonist.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
25MG | 34 | In Stock |
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50MG | 49 | In Stock |
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100MG | 73 | In Stock |
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200MG | 109 | In Stock |
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500MG | Get Quote | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameRaloxifene hydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionRaloxifeneHcl(LY156758 Hcl) is a second generation selective estrogen receptor antagonist.
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DescriptionRaloxifeneHcl(LY156758 Hcl) is a second generation selective estrogen receptor antagonist.(In Vitro):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.Raloxifene is a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, exhibits Ki values of 0.87 to 1.4 nM.Raloxifene is also a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki value of 51 nM.Raloxifene (0-80 μM; 48 hours) significantly decreased in mouse mammary carcinoma BJMC3879luc2 cells viability as a concentration manner in BJMC3879luc2 cells.(In Vivo):Raloxifene (3 mg/kg; once daily) 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.Raloxifene (oral administration; 0.1 mg/kg-10 mg/kg; 5 weeks) increases bone mineral density in the distal femur and proximal tibia. It reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat.Raloxifene (subcutaneously implanted mini-osmotic pumps; 18 or 27 mg/kg; once daily; 6 weeks) significantly suppresses tumor volumes in mice, in addition, the multiplicity of lymph node metastasis is also significantly decreased. .
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In VitroRaloxifene 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.Raloxifene is a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, exhibits Ki values of0.87 to 1.4 nM.Raloxifene is also a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki value of 51 nM.Raloxifene (0-80 μM; 48 hours) significantly decreased in mouse mammary carcinoma BJMC3879luc2 cells viability as a concentration manner in BJMC3879luc2 cells. Cell Viability Assay Cell Line:BJMC3879luc2 cells?Concentration:0 μM, 10 μM, 20 μM, 40 μM, 80 μM Incubation Time:48 hours Result:Reduced BJMC3879luc2 cell viability.
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In VivoRaloxifene (3 mg/kg; once daily) 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.Raloxifene (oral administration; 0.1 mg/kg-10 mg/kg; 5 weeks) increases bone mineral density in the distal femur and proximal tibia. It reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat.Raloxifene (subcutaneously implanted mini-osmotic pumps; 18 or 27 mg/kg; once daily; 6 weeks) significantly suppresses tumor volumes in mice, in addition, the multiplicity of lymph node metastasis is also significantly decreased.. Animal Model:Syngeneic BALB/c mice with BJMC3879luc2 cells Dosage:18 or 27 mg/kg Administration:Subcutaneously implanted mini-osmotic pumps Result:Inhibited tumor growth in mice.
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SynonymsKeoxifene | LY156758
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PathwayEndocrinology/Hormones
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TargetEstrogen Receptor/ERR
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RecptorER| AO| SERM
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Research AreaEndocrinology
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Indication——
Chemical Information
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CAS Number82640-04-8
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Formula Weight510.04
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Molecular FormulaC28H28ClNO4S
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Purity>98% (HPLC)
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SolubilityDMSO: 102 mg/mL (199.98 mM)
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SMILES[H+].[Cl-].OC1=CC=C(C=C1)C1=C(C(=O)C2=CC=C(OCCN3CCCCC3)C=C2)C2=CC=C(O)C=C2S1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Obach RS, et al. Drug Metab Dispos, 2004, 32(1), 89-97.
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