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Endoxifen (Z-isomer)

Name: Endoxifen (Z-isomer)
Brand: TargetMol
SKU: T2280
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2280Cas No. 112093-28-4

Alias Endoxifen Z-isomer

Endoxifen Z-isomer (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.

Endoxifen (Z-isomer)

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Purity: 99.81%

Catalog No. T2280Alias Endoxifen Z-isomerCas No. 112093-28-4

Endoxifen Z-isomer (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$64	In Stock	In Stock
10 mg	$85	In Stock	In Stock
25 mg	$179	In Stock	In Stock
50 mg	$288	In Stock	In Stock
100 mg	$432	-	In Stock
200 mg	$626	-	In Stock
1 mL x 10 mM (in DMSO)	$73	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:99.81%

Color:White

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COA LCMS HPLC

Product Introduction

Endoxifen (Z-isomer) AI Summary

Endoxifen (Z-isomer) demonstrates multifaceted bioactive properties. It exhibits inhibitory effects on Protein Kinase C (PKC) with a higher potency at increased concentrations, achieving 78.0% inhibition at 0.2 mM after 90 minutes. It shows significant binding affinity to bovine serum albumin, altering its secondary structure and indicating potential impacts on protein function. The compound inhibits human recombinant placental aromatase with an IC50 of 6000.0 nM and displays a high affinity for ERalpha with a fold change value of 100 relative to tamoxifen. In human MCF7:WS8 cells, it acts as an estrogen receptor agonist, enhancing PgR gene expression and ER-alpha protein levels. It also affects drug uptake in MDR1A-deficient mouse brain and interacts with efflux transporters, influencing drug delivery and pharmacokinetics. Additionally, Endoxifen (Z-isomer) exhibits antiestrogenic activity, selectively inhibiting beta-estradiol-induced progesterone receptor mRNA expression. Its antiviral properties are notable, showing efficacy against Ebolavirus entry in HeLa cells and inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells. Furthermore, Endoxifen (Z-isomer) inhibits human HDAC6, suggesting a broad spectrum of therapeutic potential..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Endoxifen Z-isomer (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.
Targets&IC50	ERG (human):1.6 μM
Synonyms	Endoxifen Z-isomer

Chemical Properties

Molecular Weight	373.49
Formula	C₂₅H₂₇NO₂
Cas No.	112093-28-4
Smiles	CC\C(=C(/c1ccc(O)cc1)c1ccc(OCCNC)cc1)c1ccccc1
Relative Density.	1.099g/cm3

Storage & Solubility Information

Storage

store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (120.49 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.35 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	2.6774 mL	13.3872 mL	26.7745 mL	133.8724 mL
5 mM	0.5355 mL	2.6774 mL	5.3549 mL	26.7745 mL
10 mM	0.2677 mL	1.3387 mL	2.6774 mL	13.3872 mL
20 mM	0.1339 mL	0.6694 mL	1.3387 mL	6.6936 mL
50 mM	0.0535 mL	0.2677 mL	0.5355 mL	2.6774 mL
100 mM	0.0268 mL	0.1339 mL	0.2677 mL	1.3387 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