Art. -Nr.: HY-103457

Y134

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Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (K_i=0.09 nM) over ERβ (K_i=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells.

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Reinheit: 99.67%
CAS. Nr.: 849662-80-2
Formel: C₂₈H₂₈N₂O₃S
Molecular Weight:472.60

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Y134 Chemical Structure

CAS. Nr.: 849662-80-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ERα

0.09 nM (Ki)

ERβ

11.31 nM (Ki)

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

In Vitro

Y134 exhibits potent antagonist activity at ERs in CV-1 cells cotransfected with plasmids containing ERα or ERβ and oestrogen-response element-driven luciferase, with IC₅₀s of 0.52 nM for ERα and 2.94 nM for ERβ^[1].
Y134 (0.01 nM-10 μM; 6 d) inhibits the oestrogen-stimulated ER-expressing breast cancer cell (MCF-7 and T47D) proliferation^[1].

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

Cell Viability Assay^[1]

Cell Line:

MCF-7, T47, MDA-MB-231 cells
Concentration:

0.01 nM-10 μM
Incubation Time:

6 days
Result:

Suppressed oestrogen-stimulated MCF-7 and T47D cell proliferation.
Showed no effects on MDA-MB-231 cells, except some cytotoxicity was seen at high concentrations.

In Vivo

Y134 (1-3 mg/kg/day; p.o. for 3 days) abolishes the E₂-induced mammary gland terminal end bud (TEB) outgrowth in ovariectomized rats. Y134 inhibits uterine cell proliferation induced by E₂ in a dose-dependent manner^[1].

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

Animal Model:

Four-week old female Sprague-Dawley rats were received ovariectomy^[1]
Dosage:

1, 3 mg/kg
Administration:

P.o. daily for 3 days
Result:

Abolished the effect exerted by E2 in a dose-dependent manner.

Chemical Information

CAS. Nr. 849662-80-2
Appearance Solid
Molecular Weight 472.60
Formel C₂₈H₂₈N₂O₃S
Color Light yellow to yellow
SMILES

O=C(C1=C(C2=CC=C(O)C=C2)SC3=CC(O)=CC=C31)C4=CC=C(N5CCN(C(C)C)CC5)C=C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (211.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1160 mL

10.5798 mL

21.1595 mL

5 mM

0.4232 mL

2.1160 mL

4.2319 mL

10 mM

0.2116 mL

1.0580 mL

2.1160 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (5.29 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.29 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.29 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

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

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ning M, et, al. Biological activities of a novel selective oestrogen receptor modulator derived from raloxifene (Y134). Br J Pharmacol. 2007 Jan;150(1):19-28. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
DMSO	1 mM	2.1160 mL	10.5798 mL	21.1595 mL	52.8989 mL
	5 mM	0.4232 mL	2.1160 mL	4.2319 mL	10.5798 mL
	10 mM	0.2116 mL	1.0580 mL	2.1160 mL	5.2899 mL
	15 mM	0.1411 mL	0.7053 mL	1.4106 mL	3.5266 mL
	20 mM	0.1058 mL	0.5290 mL	1.0580 mL	2.6449 mL
	25 mM	0.0846 mL	0.4232 mL	0.8464 mL	2.1160 mL
	30 mM	0.0705 mL	0.3527 mL	0.7053 mL	1.7633 mL
	40 mM	0.0529 mL	0.2645 mL	0.5290 mL	1.3225 mL
	50 mM	0.0423 mL	0.2116 mL	0.4232 mL	1.0580 mL
	60 mM	0.0353 mL	0.1763 mL	0.3527 mL	0.8816 mL
	80 mM	0.0264 mL	0.1322 mL	0.2645 mL	0.6612 mL
	100 mM	0.0212 mL	0.1058 mL	0.2116 mL	0.5290 mL

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Y134

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Y134

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Y134 Related Classifications

HY-103457 Related Classifications