Raloxifene (hydrochloride) [82640-04-8]
Référence HY-13738A-100mg
Conditionnement : 100mg
Marque : MedChemExpress
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.
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Raloxifene hydrochloride Chemical Structure
CAS No. : 82640-04-8
This product is a controlled substance and not for sale in your territory.
Based on 9 publication(s) in Google Scholar
Other Forms of Raloxifene hydrochloride:
- Raloxifene In-stock
- Raloxifene hydrochloride (Standard) In-stock
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] |
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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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability Assay[5]
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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].. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Essai clinique |
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Masse moléculaire |
510.04 |
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Formule |
C28H28ClNO4S |
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CAS No. |
82640-04-8 |
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Appearance |
Solid |
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Color |
Light yellow to yellow |
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SMILES |
O=C(C1=C(C2=CC=C(O)C=C2)SC3=CC(O)=CC=C31)C4=CC=C(OCCN5CCCCC5)C=C4.Cl |
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Structure Classification |
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Initial Source |
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Livraison | Room temperature in continental US; may vary elsewhere. |
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Stockage |
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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Solvant et solubilité |
In Vitro:
DMSO : 33.33 mg/mL (65.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O : < 0.1 mg/mL (insoluble) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
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 Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Pureté et documentation | |||||||||||||
Références |
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Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 1.9606 mL | 9.8032 mL | 19.6063 mL | 49.0158 mL |
5 mM | 0.3921 mL | 1.9606 mL | 3.9213 mL | 9.8032 mL | |
10 mM | 0.1961 mL | 0.9803 mL | 1.9606 mL | 4.9016 mL | |
15 mM | 0.1307 mL | 0.6535 mL | 1.3071 mL | 3.2677 mL | |
20 mM | 0.0980 mL | 0.4902 mL | 0.9803 mL | 2.4508 mL | |
25 mM | 0.0784 mL | 0.3921 mL | 0.7843 mL | 1.9606 mL | |
30 mM | 0.0654 mL | 0.3268 mL | 0.6535 mL | 1.6339 mL | |
40 mM | 0.0490 mL | 0.2451 mL | 0.4902 mL | 1.2254 mL | |
50 mM | 0.0392 mL | 0.1961 mL | 0.3921 mL | 0.9803 mL | |
60 mM | 0.0327 mL | 0.1634 mL | 0.3268 mL | 0.8169 mL |
Raloxifene hydrochloride Related Classifications
- Vitamin D Related/Nuclear Receptor Autophagy
- Estrogen Receptor/ERR Autophagy