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Y134

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Catalog No. T23540Cas No. 849662-80-2
Alias Y 134

Y134 is an estrogen receptor inhibitor that is selective and orally active, exhibiting strong antagonist activity against ERα and Erβ with Ki of 0.09 nM and 11.31 nM, respectively. The selectivity of Y134 for ERα is 121.1 times higher than that for ERβ. Y134 inhibited the proliferation of ER positive human breast cancer cells stimulated by estrogen.

Y134

Y134

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Purity: 99.98%
Catalog No. T23540Alias Y 134Cas No. 849662-80-2
Y134 is an estrogen receptor inhibitor that is selective and orally active, exhibiting strong antagonist activity against ERα and Erβ with Ki of 0.09 nM and 11.31 nM, respectively. The selectivity of Y134 for ERα is 121.1 times higher than that for ERβ. Y134 inhibited the proliferation of ER positive human breast cancer cells stimulated by estrogen.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$38In StockIn Stock
5 mg$94In StockIn Stock
10 mg$153In StockIn Stock
25 mg$308In StockIn Stock
50 mg$461In StockIn Stock
100 mg$738-In Stock
200 mg$1,000-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.98%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
Y134 is an estrogen receptor inhibitor that is selective and orally active, exhibiting strong antagonist activity against ERα and Erβ with Ki of 0.09 nM and 11.31 nM, respectively. The selectivity of Y134 for ERα is 121.1 times higher than that for ERβ. Y134 inhibited the proliferation of ER positive human breast cancer cells stimulated by estrogen.
Targets&IC50
ERβ:11.31 nM (Ki), ERα:0.09 nM (Ki)
In vitro
Y134 displays robust antagonistic effects on estrogen receptors (ERs) in CV-1 cells co-transfected with plasmids carrying ERα or ERβ along with estrogen-response element-driven luciferase, resulting in a significant decrease in luciferase activity.[1]
Treatment with Y134 (0.01 nM-10 μM; 6 d) effectively suppresses the proliferation of ER-expressing breast cancer cells (MCF-7 and T47D) stimulated by estrogen.[1]
In vivo
Administration of Y134 (1-3 mg/kg/day; p.o. for 3 days) completely eliminates the estrogen-induced growth of terminal end buds (TEB) in the mammary glands of ovariectomized rats. Y134 exhibits a dose-dependent inhibition of uterine cell proliferation induced by estrogen (E2). [1]
SynonymsY 134
Chemical Properties
Molecular Weight472.6
FormulaC28H28N2O3S
Cas No.849662-80-2
SmilesC(=O)(C1=C(SC=2C1=CC=C(O)C2)C3=CC=C(O)C=C3)C4=CC=C(C=C4)N5CCN(C(C)C)CC5
Relative Density.1.282g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 47.26 mg/mL (100 mM), Sonication is recommended.
Ethanol: 47.26 mg/mL (100 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4.23 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/Ethanol
1mg5mg10mg50mg
1 mM2.1160 mL10.5798 mL21.1595 mL105.7977 mL
5 mM0.4232 mL2.1160 mL4.2319 mL21.1595 mL
10 mM0.2116 mL1.0580 mL2.1160 mL10.5798 mL
20 mM0.1058 mL0.5290 mL1.0580 mL5.2899 mL
50 mM0.0423 mL0.2116 mL0.4232 mL2.1160 mL
100 mM0.0212 mL0.1058 mL0.2116 mL1.0580 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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