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Raloxifene hydrochloride

Name: Raloxifene hydrochloride
Brand: TargetMol
SKU: T1549
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1549Cas No. 82640-04-8

Alias Raloxifene HCl, LY156758 hydrochloride, LY156758 (Keoxifene) HCl, LY139481 hydrochloride, Keoxifene hydrochloride

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Raloxifene hydrochloride

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Purity: 99.97%

Catalog No. T1549Alias Raloxifene HCl, LY156758 hydrochloride, LY156758 (Keoxifene) HCl, LY139481 hydrochloride, Keoxifene hydrochlorideCas No. 82640-04-8

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$38	In Stock	In Stock
50 mg	$54	In Stock	In Stock
100 mg	$81	In Stock	In Stock
200 mg	$121	In Stock	In Stock
500 mg	$196	-	In Stock
1 mL x 10 mM (in DMSO)	$58	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.97%

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.
Targets&IC50	ER:5.7 nM
In vitro	Raloxifene significantly differs from estrogen due to its lack of substantial estrogenic effects on uterine tissues. In rat femurs, Raloxifene rebuilds bone mineral density and the expression of TGF beta 3 mRNA. Oral administration of 0.1 mg/kg to 10 mg/kg of Raloxifene for 5 weeks increases the density of femurs and tibias in ovariectomized rats. With an ED50 of 0.2 mg/kg, Raloxifene reduces serum cholesterol levels in ovariectomized (OVX) rats. In ovariectomized rats, Raloxifene blocks the deterioration of bone quality and growth changes, bone remodeling, and serum cholesterol content, albeit with lesser effects on reducing bone formation and unable to prevent uterine atrophy.
In vivo	Raloxifene is a non-competitive inhibitor of aldehyde oxidase (with a Ki of 51 nM), targeting the enzyme's reduction reaction of compounds containing isohydroxystearic acid. It has been proven to effectively inhibit the human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-δ1' (5')- iminium with Ki values of 0.87 nM, 1.2 nM, and 1.4 nM, respectively. Additionally, Raloxifene acts as a full agonist at nanomolar concentrations, activating the TGFβ 3 promoter, and serves as a pure estrogen antagonist in transient transfection assays by inhibiting the expression of vitellogenin promoter with estrogen response elements.
Synonyms	Raloxifene HCl, LY156758 hydrochloride, LY156758 (Keoxifene) HCl, LY139481 hydrochloride, Keoxifene hydrochloride

Chemical Properties

Molecular Weight	510.044
Formula	C₂₈H₂₈ClNO₄S
Cas No.	82640-04-8
Smiles	Cl.Oc1ccc(cc1)-c1sc2cc(O)ccc2c1C(=O)c1ccc(OCCN2CCCCC2)cc1
Relative Density.	1.285g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 245 mg/mL (480.35 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.92 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9606 mL	9.8031 mL	19.6062 mL	98.0308 mL
5 mM	0.3921 mL	1.9606 mL	3.9212 mL	19.6062 mL
10 mM	0.1961 mL	0.9803 mL	1.9606 mL	9.8031 mL
20 mM	0.0980 mL	0.4902 mL	0.9803 mL	4.9015 mL
50 mM	0.0392 mL	0.1961 mL	0.3921 mL	1.9606 mL
100 mM	0.0196 mL	0.0980 mL	0.1961 mL	0.9803 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc