SR1001
Based on 7 publication(s) in Google Scholar
SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 1335106-03-0
- Formula: C15H13F6N3O4S2
- Molecular Weight:477.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SR1001
More- J Neuroinflammation. 2025 Aug 26;22(1):207. [Abstract]
- J Neuroinflammation. 2022 Jul 14;19(1):186. [Abstract]
- Cell Rep. 2024 Feb 15;43(2):113786. [Abstract]
- Commun Biol. 2026 Jan 13;9(1):247. [Abstract]
- J Nutr Biochem. 2023 Jan:111:109155. [Abstract]
- Int Immunopharmacol. 2022 Aug:109:108778. [Abstract]
- FASEB J. 2019 Apr;33(4):5704-5715. [Abstract]
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
4 μM
Compound: SR1001
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Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay
Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay
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10.1039/C3MD00005B |
| HEK293 | EC50 |
4 μM
Compound: SR1001
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Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay
Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay
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10.1039/C3MD00005B |
SR1001 inhibits the development of murine TH17 cells by inhibition of IL-17A gene expression and protein production. SR1001 reduces the interaction of a coactivator TRAP220 NR box 2 peptide with RORγ in a dose dependent manner (IC50 value≈117 nM). Additionally, SR1001 inhibits the expression of cytokines when added to differentiated murine or human TH17 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1335106-03-0
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Appearance Solid
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Molecular Weight 477.40
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Formula C15H13F6N3O4S2
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Color White to yellow
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SMILES
CC(NC1=NC(C)=C(S(=O)(NC2=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C2)=O)S1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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J Neuroinflammation
Disrupted betaine metabolism drives Th17 cell differentiation, mediating methamphetamine-induced depressive behaviors in male mice. [Abstract]2025 Aug 26;22(1):207. PMID: 40859333 -
J Neuroinflammation
Chronic stress-induced depression requires the recruitment of peripheral Th17 cells into the brain. [Abstract]2022 Jul 14;19(1):186. PMID: 35836182 -
Cell Rep
RORα is required for expansion and memory maintenance of ILC1s via a lymph node-liver axis. [Abstract]2024 Feb 15;43(2):113786. PMID: 38363684 -
Commun Biol
Distinct effects of different Bacteroides strains on depressive-like behavior via a gut-Th1/Th17 cells-brain axis. [Abstract]2026 Jan 13;9(1):247. PMID: 41530303 -
J Nutr Biochem
Treatment with butyrate alleviates dextran sulfate sodium and Clostridium difficile-induced colitis by preventing activity of Th17 cells via regulation of SIRT1/mTOR in mice. [Abstract]2023 Jan:111:109155. PMID: 36162566 -
Int Immunopharmacol
Melatonin relieves Th17/CD4-CD8- T cells inflammatory responses via nuclear-receptor dependent manner in peripheral blood of primary Sjögren's syndrome. [Abstract]2022 Aug:109:108778. PMID: 35537347 -
FASEB J
The orphan nuclear receptor RORα is a potential endogenous protector in renal ischemia/reperfusion injury. [Abstract]2019 Apr;33(4):5704-5715. PMID: 30673513
Solvent & Solubility
DMSO : ≥ 39 mg/mL (81.69 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (4.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (4.36 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol
HEK293 cells are plated in 96-well plates at a density of 15 x 103 cells/well. Transfections are performed using Lipofectamine 2000. 24 h post-transfection, the cells are treated with vehicle or compound (SR1001). 24 h post-treatment, the luciferase activity is measured using the Dual-Glo luciferase assay system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Experimental autoimmune encephalomyelitis is induced in C57BL/6 wild-type mice by s.c. injection over four sites in the flank with 200 μg per mouse. The SR1001 is dissolved in DMSO at 25 mg/mL and the mice are treated (i.p.) with 25 mg/kg SR1001 (1 μL/g body weight of mouse) or vehicle (DMSO, 1 μL/g body weight of mouse) twice per day. The treatment is started 2 days before immunization and continued until the end of experiment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Solt LA, et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4. [Content Brief]
[2]. Crumbley C, et al. Regulation of expression of citrate synthase by the retinoic acid receptor-related orphan receptor α (RORα). PLoS One. 2012;7(4):e33804. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0947 mL | 10.4734 mL | 20.9468 mL | 52.3670 mL |
| 5 mM | 0.4189 mL | 2.0947 mL | 4.1894 mL | 10.4734 mL | |
| 10 mM | 0.2095 mL | 1.0473 mL | 2.0947 mL | 5.2367 mL | |
| 15 mM | 0.1396 mL | 0.6982 mL | 1.3965 mL | 3.4911 mL | |
| 20 mM | 0.1047 mL | 0.5237 mL | 1.0473 mL | 2.6183 mL | |
| 25 mM | 0.0838 mL | 0.4189 mL | 0.8379 mL | 2.0947 mL | |
| 30 mM | 0.0698 mL | 0.3491 mL | 0.6982 mL | 1.7456 mL | |
| 40 mM | 0.0524 mL | 0.2618 mL | 0.5237 mL | 1.3092 mL | |
| 50 mM | 0.0419 mL | 0.2095 mL | 0.4189 mL | 1.0473 mL | |
| 60 mM | 0.0349 mL | 0.1746 mL | 0.3491 mL | 0.8728 mL | |
| 80 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6546 mL |
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