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Description: Raloxifene HCl (also known as LY-156758; LY-139481; trade names: Evista; Keoxifene; RALOX), the hydrochloride salt of Raloxifene, is a selective estrogen antagonist or estrogen strogen receptor modulator (SERM) that has been approved as a medication to prevent and treat osteoporosis in postmenopausal women. It inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with an IC50 of 5.7 nM. Raloxifene belongs to the benzothiophene class of estrogen strogen receptor modulator (SERM). Raloxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist; it displays both an ER-α-selective partial agonist/antagonist effect and a pure ER-ß-selective antagonist effect.
References: Drug Metab Dispos. 2004 Jan;32(1):89-97; Endocrinology. 1996 May;137(5):2075-84.
Related CAS #: 84449-90-1 (free base); 82640-04-8 or 84449-90-1 (HCl); 174264-50-7 (6-glucuronide); 84449-82-1 (dimethyl ester HCl); 185415-07-0 (4-Monomethyl Ether); 178451-13-3 (6-Monomethyl Ether); 84541-36-6 (Raloxifene Bismethyl Ether HCl, a metabolite of Raloxifene); 84541-38-8 (Raloxifene Bismethyl Ether); 182507-22-8 (Raloxifene 4'-glucuronide); 195454-31-0 (Raloxifene N-Oxide); 182507-20-6 (Raloxifene 6,4'-Bis-β-D-glucuronide); 174264-46-1 (4'-tert-Butyldimethylsilyl-6-hydroxy Raloxifene); 334758-18-8 (6-Raloxifene-β-D-glucopyranoside); 334758-19-9 (4'-Raloxifene-β-D-glucopyranoside); 174264-51-8 [Methyl Raloxifene 4'-(2,3,4-Tri-O-acetyl-β-D-glycopyranuronate)]; 1159977-58-8 [7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene]; 177744-96-6 (LY88074); 63676-25-5 (LY117018)
Product Catalog 2022
Guide to Product Handling
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: 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. 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.
Drug Metab Dispos. 2004 Jan;32(1):89-97; Endocrinology. 1996 May;137(5):2075-84.
Purity ≥98%
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