SR1555
Based on 1 Customer Validation
SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.69%
- CAS. Nr.: 1386439-51-5
- Formel: C22H22F6N2O2
- Molecular Weight:460.41
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Biologische Aktivität
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RORγ 1 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
1.5 μM
Compound: 14, SR1555
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Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay
Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay
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[PMID: 24502334] |
| HEK-293T | IC50 |
1.5 μM
Compound: SR1555
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Inhibition of GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells assessed as suppression of transcriptional activity after 20 hrs
Inhibition of GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells assessed as suppression of transcriptional activity after 20 hrs
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10.1039/C3MD00005B |
SR1555 (10 μM; 24 h) inhibits Il17a gene expression by greater than 70%in EL4 cells[1].
SR1555 (10 μM; 24 h) inhibits IL-17 protein expression, inhibits TH17 cell differentiation and function, and does not induce cell death during TH17 cell differentiation[1].
SR1555 (10 μM; 24 h) effectively increases the gene expression of Foxp3 while simultaneously suppressing the gene expression of Rorγt[1].
SR1555 increases the frequency of T regulatory cells as evidenced by the almost 2-fold increase in the expression of Foxp3+ T cells in the splenocyte culture[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EL4 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Inhibited Il17a gene expression by greater than 70%.
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Cell Line:Splenocytes (cultured under TH17 polarizing conditions for 3 days)
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Concentration:10 μM
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Incubation Time:24 h
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Result:Inhibited IL-17 protein expression, inhibited TH17 cell differentiation and function, and did not induce cell death during TH17 cell differentiation.
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Cell Line:Splenocytes (cultured under T regulatory cell polarizing conditions for 3 days)
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Concentration:10 μM
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Incubation Time:24 h
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Result:Effectively increased the gene expression of Foxp3 while simultaneously suppressing the gene expression of Rorγt.
Chemical Information
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CAS. Nr. 1386439-51-5
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Appearance Solid
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Molecular Weight 460.41
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Formel C22H22F6N2O2
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Color White to light yellow
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SMILES
CC(N1CCN(CC2=CC=C(C3=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C3)C=C2)CC1)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (217.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.43 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 (5.43 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.
Reinheit & Dokumentation
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Data Sheet (273 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)
Verweise
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 | 2.1720 mL | 10.8599 mL | 21.7198 mL | 54.2994 mL |
| 5 mM | 0.4344 mL | 2.1720 mL | 4.3440 mL | 10.8599 mL | |
| 10 mM | 0.2172 mL | 1.0860 mL | 2.1720 mL | 5.4299 mL | |
| 15 mM | 0.1448 mL | 0.7240 mL | 1.4480 mL | 3.6200 mL | |
| 20 mM | 0.1086 mL | 0.5430 mL | 1.0860 mL | 2.7150 mL | |
| 25 mM | 0.0869 mL | 0.4344 mL | 0.8688 mL | 2.1720 mL | |
| 30 mM | 0.0724 mL | 0.3620 mL | 0.7240 mL | 1.8100 mL | |
| 40 mM | 0.0543 mL | 0.2715 mL | 0.5430 mL | 1.3575 mL | |
| 50 mM | 0.0434 mL | 0.2172 mL | 0.4344 mL | 1.0860 mL | |
| 60 mM | 0.0362 mL | 0.1810 mL | 0.3620 mL | 0.9050 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2715 mL | 0.6787 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2172 mL | 0.5430 mL |
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