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  3. Raloxifene hydrochloride

Raloxifene hydrochloride (Synonyms: Keoxifene hydrochloride; LY156758; LY139481 hydrochloride)

Cat. No.: HY-13738A Purity: 99.94%
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Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.

For research use only. We do not sell to patients.

Raloxifene hydrochloride Chemical Structure

Raloxifene hydrochloride Chemical Structure

CAS No. : 82640-04-8

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10 mM * 1 mL in DMSO USD 66 In-stock
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100 mg USD 96 In-stock
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Based on 3 publication(s) in Google Scholar

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Description

Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue[1].

IC50 & Target

IC50: estrogen receptor[1]

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[1].
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[2].
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[2].
Raloxifene (0-80 μM; 48 hours) significantly decreased in mouse mammary carcinoma BJMC3879luc2 cells viability as a concentration manner in BJMC3879luc2 cells[5].

Cell Viability Assay[5]

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[3].
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[4].
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[5].
.

Animal Model: Syngeneic BALB/c mice with BJMC3879luc2 cells[5]
Dosage: 18 or 27 mg/kg
Administration: Subcutaneously implanted mini-osmotic pumps
Result: Inhibited tumor growth in mice.
Clinical Trial
Molecular Weight

510.04

Formula

C₂₈H₂₈ClNO₄S

CAS No.

82640-04-8

SMILES

O=C(C1=C(C2=CC=C(O)C=C2)SC3=CC(O)=CC=C31)C4=CC=C(OCCN5CCCCC5)C=C4.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (65.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9606 mL 9.8032 mL 19.6063 mL
5 mM 0.3921 mL 1.9606 mL 3.9213 mL
10 mM 0.1961 mL 0.9803 mL 1.9606 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

RaloxifeneKeoxifeneLY156758LY139481LY 156758LY-156758LY 139481LY-139481Estrogen Receptor/ERRAutophagyInhibitorinhibitorinhibit

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Raloxifene hydrochloride
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