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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
25MG 34 In Stock
50MG 49 In Stock
100MG 73 In Stock
200MG 109 In Stock
500MG Get Quote In Stock
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Biological Information

  • Product Name
    Raloxifene hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    RaloxifeneHcl(LY156758 Hcl) is a second generation selective estrogen receptor antagonist.
  • Description
    RaloxifeneHcl(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. .
  • 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 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.
  • 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.. 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.
  • Synonyms
    Keoxifene | LY156758
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    ER| AO| SERM
  • Research Area
    Endocrinology
  • Indication
    ——

Chemical Information

  • CAS Number
    82640-04-8
  • Formula Weight
    510.04
  • Molecular Formula
    C28H28ClNO4S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 102 mg/mL (199.98 mM)
  • SMILES
    [H+].[Cl-].OC1=CC=C(C=C1)C1=C(C(=O)C2=CC=C(OCCN3CCCCC3)C=C2)C2=CC=C(O)C=C2S1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Obach RS, et al. Drug Metab Dispos, 2004, 32(1), 89-97.
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