Estrogen receptor-IN-1
Based on 1 publication(s) in Google Scholar
Estrogen receptor-IN-1 (compound 16) is a potent estrogen receptor (ER) inhibitor with IC50s of 13, 5µM for ERα and Erβ, respectively.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 74027-99-9
- Formula: C14H16OSi
- Molecular Weight:228.36
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Storage:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Estrogen receptor-IN-1
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Biological Activity
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ERα 13 μM (IC50) |
ERβ 5 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>30 μM
Compound: 16
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Agonist activity at human Gal4-fused ERalpha expressed in HEK293 cells assessed as transcriptional activation after 24 hrs by luciferase/beta-galactosidase reporter gene assay
Agonist activity at human Gal4-fused ERalpha expressed in HEK293 cells assessed as transcriptional activation after 24 hrs by luciferase/beta-galactosidase reporter gene assay
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[PMID: 31980362] |
| HEK293 | IC50 |
13 μM
Compound: 16
|
Antagonist activity at human Gal4-fused ERalpha expressed in HEK293 cells assessed as inhibition of E2-induced transcriptional activation after 24 hrs by luciferase/beta-galactosidase reporter gene assay
Antagonist activity at human Gal4-fused ERalpha expressed in HEK293 cells assessed as inhibition of E2-induced transcriptional activation after 24 hrs by luciferase/beta-galactosidase reporter gene assay
|
[PMID: 31980362] |
| HEK293 | IC50 |
5 μM
Compound: 16
|
Antagonist activity at human Gal4-fused ERbeta expressed in HEK293 cells assessed as inhibition of E2-induced transcriptional activation after 24 hrs by luciferase/beta-galactosidase reporter gene assay
Antagonist activity at human Gal4-fused ERbeta expressed in HEK293 cells assessed as inhibition of E2-induced transcriptional activation after 24 hrs by luciferase/beta-galactosidase reporter gene assay
|
[PMID: 31980362] |
| MCF7 | EC50 |
16 nM
Compound: 16
|
Estrogenic activity in human MCF7 cells assessed as cell proliferation after 7 days by WST-8 assay
Estrogenic activity in human MCF7 cells assessed as cell proliferation after 7 days by WST-8 assay
|
[PMID: 23214428] |
Chemical Information
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CAS No. 74027-99-9
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Appearance Oil
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Molecular Weight 228.36
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Formula C14H16OSi
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Color Colorless to light yellow
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SMILES
OC1=CC=C([Si](C)(C)C2=CC=CC=C2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep
Bisphenol S induces brown adipose tissue whitening and aggravates diet-induced obesity in an estrogen-dependent manner. [Abstract]2023 Dec 1;42(12):113504. PMID: 38041811
Solvent & Solubility
DMSO : ≥ 100 mg/mL (437.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.95 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.95 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Purity & Documentation
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Data Sheet (271 KB)
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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)
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Handling Instructions (2659 KB)
References
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. 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 | 4.3791 mL | 21.8953 mL | 43.7905 mL | 109.4763 mL |
| 5 mM | 0.8758 mL | 4.3791 mL | 8.7581 mL | 21.8953 mL | |
| 10 mM | 0.4379 mL | 2.1895 mL | 4.3791 mL | 10.9476 mL | |
| 15 mM | 0.2919 mL | 1.4597 mL | 2.9194 mL | 7.2984 mL | |
| 20 mM | 0.2190 mL | 1.0948 mL | 2.1895 mL | 5.4738 mL | |
| 25 mM | 0.1752 mL | 0.8758 mL | 1.7516 mL | 4.3791 mL | |
| 30 mM | 0.1460 mL | 0.7298 mL | 1.4597 mL | 3.6492 mL | |
| 40 mM | 0.1095 mL | 0.5474 mL | 1.0948 mL | 2.7369 mL | |
| 50 mM | 0.0876 mL | 0.4379 mL | 0.8758 mL | 2.1895 mL | |
| 60 mM | 0.0730 mL | 0.3649 mL | 0.7298 mL | 1.8246 mL | |
| 80 mM | 0.0547 mL | 0.2737 mL | 0.5474 mL | 1.3685 mL | |
| 100 mM | 0.0438 mL | 0.2190 mL | 0.4379 mL | 1.0948 mL |