Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

Raloxifene (hydrochloride) [82640-04-8]

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Cat# HY-13738A-100mg

Size : 100mg

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Marca : MedChemExpress

Contatta il distributore locale :

Telefono : +1 850 650 7790

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

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Description

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 K_i 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 K_i 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]

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].
.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Essai clinique

Masse moléculaire

510.04

Formule

C₂₈H₂₈ClNO₄S

CAS No.

82640-04-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Structure Classification

Alkaloids
Piperidine Alkaloids

Phenols
Polyphenols

Initial Source

Plants
Rutaceae
Tetradium ruticarpum (A. Jussieu) T. G. Hartley

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

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

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.
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.

Calculateur de molarité
Calculateur de dilution

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:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

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

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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.

Pureté et documentation

Purity: 99.78%

Select Batch:

Fiche technique (283 KB) SDS (393 KB)

COA (256 KB) RP-HPLC (246 KB) LCMS (270 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Yang, N.N., et al., Estrogen and raloxifene stimulate transforming growth factor-beta 3 gene expression in rat bone: a potential mechanism for estrogen- or raloxifene-mediated bone maintenance. Endocrinology, 1996. 137(5): p. 2075-84. [Content Brief]

[2]. Obach, R.S., Potent inhibition of human liver aldehyde oxidase by raloxifene. Drug Metab Dispos, 2004. 32(1): p. 89-97. [Content Brief]

[3]. Sato, M., M.K. Rippy, and H.U. Bryant, Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. FASEB J, 1996. 10(8): p. 905-12. [Content Brief]

[4]. Black, L.J., et al., Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin Invest, 1994. 93(1): p. 63-9. [Content Brief]

[5]. Shibata MA, et al. Raloxifene inhibits tumor growth and lymph node metastasis in a xenograft model of metastatic mammary cancer.BMC Cancer. 2010 Oct 19;10:566. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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

Raloxifene (hydrochloride) [82640-04-8]

Cat# HY-13738A-100mg

Contatta il distributore locale :

Marca : MedChemExpress

Contatta il distributore locale :

Other Forms of Raloxifene hydrochloride:

Voir tous les produits spécifiques à Isoform Estrogen Receptor/ERR:

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Raloxifene hydrochloride Related Classifications

Keywords:

Si può anche essere interessati nei seguenti prodotti:

Raloxifene (hydrochloride) [82640-04-8]

Cat# HY-13738A-100mg

Contatta il distributore locale :

Marca : MedChemExpress

Contatta il distributore locale :

Other Forms of Raloxifene hydrochloride:

Voir tous les produits spécifiques à Isoform Estrogen Receptor/ERR:

Raloxifene hydrochloride Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Raloxifene hydrochloride Related Classifications

Keywords:

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