SR3335
Based on 14 publication(s) in Google Scholar
SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.49%
- CAS. Nr.: 293753-05-6
- Formel: C13H9F6NO3S2
- Molecular Weight:405.34
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) SR3335
More- Nat Commun. 2024 Jun 13;15(1):5056. [Abstract]
- Cell Death Dis. 2021 Sep 28;12(10):886. [Abstract]
- NPJ Parkinsons Dis. 2022 Jul 8;8(1):90. [Abstract]
- Antioxidants (Basel). 2022 Apr 8;11(4):748. [Abstract]
- J Pineal Res. 2019 Sep;67(2):e12581. [Abstract]
- FASEB J. 2026 Jun 15;40(11):e71983. [Abstract]
- Mediators Inflamm. 2021 Jul 28:2021:9954909. [Abstract]
- Poultry Sci. 2020 Sep;99(9):4294-4302. [Abstract]
- Cell Signal. 2023 Jul:107:110678. [Abstract]
- Eur J Med Res. 2025 Nov 5;30(1):1073. [Abstract]
- Immunol Res. 2024 Jun;72(3):383-394. [Abstract]
- Cell Immunol. 2024 Aug 15:403-404:104862. [Abstract]
- Immunol Lett. 2019 Sep:213:21-29. [Abstract]
- Res Vet Sci. 2025 Oct:194:105823. [Abstract]
Biologische Aktivität
Ki: 220 nM (RORα)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
480 nM
Compound: SR3335
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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 |
SR3335 is a selective RORα partial inverse agonist. In a biochemical radioligand binding assay using [3H]25-hydroxycholesterol as a label it is clear that unlabeled SR3335 dose-dependently competes for binding to the RORα LBD. The Ki is calculated as 220 nM using the Cheng-Prusoff equation. In a cell-based chimeric receptor Gal4 DNA-binding domain-NR ligand binding domain cotransfection assay, SR3335 significantly inhibits the constitutive transactivation activity of RORα (IC50=480 nM)(partial inverse agonist activity), but has no effect on the activity of LXRα and RORγ[1].
SR3335 suppresses the expression of endogenous RORα target genes in HepG2 cells that are involved in hepatic gluconeogenesis including glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK)[2].
SR3335 also blocks IL-25 and IL-33-induced ILC2 proliferation and IL-13 production ex vivo[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SR3335 (15 mg/kg/day; ip for 7 days) reduces rhinovirus (RV)-induced lung ILC2s in immature mice (RV infection of 6-day-old BALB/c mice)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 293753-05-6
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Appearance Solid
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Molecular Weight 405.34
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Formel C13H9F6NO3S2
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Color White to off-white
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SMILES
O=S(C1=CC=CS1)(NC2=CC=C(C(C(F)(F)F)(C(F)(F)F)O)C=C2)=O
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Synonyms
ML 176
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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
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Commun
2024 Jun 13;15(1):5056. PMID: 38871792 -
Cell Death Dis
Inhibition of nuclear receptor RORα attenuates cartilage damage in osteoarthritis by modulating IL-6/STAT3 pathway. [Abstract]2021 Sep 28;12(10):886. PMID: 34584074 -
NPJ Parkinsons Dis
Melatonin ameliorates Parkinson's disease via regulating microglia polarization in a RORα-dependent pathway. [Abstract]2022 Jul 8;8(1):90. PMID: 35803929 -
Antioxidants (Basel)
Melatonin Nuclear Receptors Mediate Green-and-Blue-Monochromatic-Light-Combinations-Inhibited B Lymphocyte Apoptosis in the Bursa of Chickens via Reducing Oxidative Stress and Nfκb Expression. [Abstract]2022 Apr 8;11(4):748. PMID: 35453433 -
J Pineal Res
Melatonin stabilizes rupture-prone vulnerable plaques via regulating macrophage polarization in a nuclear circadian receptor RORα-dependent manner. [Abstract]2019 Sep;67(2):e12581. PMID: 31009101 -
FASEB J
Retinoic Acid-Related Orphan Nuclear Receptor Alpha Promotes Cartilage Degeneration in Osteoarthritis by Activating the Wnt/β-Catenin Pathway. [Abstract]2026 Jun 15;40(11):e71983. PMID: 42240585 -
Mediators Inflamm
Inverse Agonist of Retinoid-Related Orphan Receptor-Alpha Prevents Apoptosis and Degeneration in Nucleus Pulposus Cells via Upregulation of YAP. [Abstract]2021 Jul 28:2021:9954909. PMID: 34366712 -
Poultry Sci
Melatonin mediates monochromatic light-induced proliferation of T/B lymphocytes in the spleen via the membrane receptor or nuclear receptor. [Abstract]2020 Sep;99(9):4294-4302. PMID: 32867973 -
Cell Signal
MicroRNA-155 suppressed cholesterol-induced matrix degradation, pyroptosis and apoptosis by targeting RORα in nucleus pulposus cells. [Abstract]2023 Jul:107:110678. PMID: 37062437 -
Eur J Med Res
Retinoic acid-related orphan nuclear receptor alpha inhibits adipogenic differentiation of bone marrow mesenchymal stem cells via activating WNT/β-catenin signaling pathway. [Abstract]2025 Nov 5;30(1):1073. PMID: 41194142 -
Immunol Res
2024 Jun;72(3):383-394. PMID: 38265549 -
Cell Immunol
2024 Aug 15:403-404:104862. PMID: 39159505 -
Immunol Lett
Effect of the melatonin nuclear receptor RORα on monochromatic light-induced T-lymphocyte proliferation in chicken thymus. [Abstract]2019 Sep:213:21-29. PMID: 31326445 -
Res Vet Sci
Melatonin improves growth and slaughter performance of broilers by regulating satellite cell proliferation via RORα nuclear receptor. [Abstract]2025 Oct:194:105823. PMID: 40737973
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (246.71 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.
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 (6.17 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 (6.17 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 10 mg/mL (24.67 mM); Clear solution; Need ultrasonic
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.
Protokoll
HEK293 cells are maintained in Dulbecco’s modified Eagle’s medium (DMEM) supplemented with 10% fetal bovine serum at 37°C under 5% CO2. HepG2 cells are maintained and routinely propagated in minimum essential medium supplemented with 10% fetal bovine serum at 37°C under 5% CO2. 24 h prior to transfection, cells are plated in 96-well plates at a density of 15×103 cells/well. Transfections are performed using LipofectamineTM 2000. 16 h post-transfection, the cells are treated with vehicle or SR3335. 24 h post-treatment, the luciferase activity is measured using the Dual-GloTM luciferase assay system. The values indicated represent the means±S.E. from four independently transfected wells. The experiments are repeated at least three times[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
30 week old Diet induced obese (DIO) C57BL/6 male mice are purchased from Jackson Laboratories that are maintained on a 65% Kcal high-fat diet from weaning. DIO mice are treated twice per day (07:00h and 18:00h) with 15 mg/kg SR3335 or vehicle for 6 days i.p. Pyruvate tolerance test is conducted on day 6 of the treatment. Food is removed from mice in the morning after SR3335 injection, fasted for 6 hours and the pyruvate tolerance test is conducted at 13:00h. Time 0 blood glucose is measured taken from the tail nip and the pyruvate challenge is initiated by injection of 2g/kg of pyruvate i.p. followed by measuring blood glucose at 15, 30 and 60 min following the injection. Blood glucose is measured by one touch ultra glucose-meter.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Kumar N, et al. Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist. ACS Chem Biol. 2011 Mar 18;6(3):218-22. [Content Brief]
[2]. Rajput C, et al. RORα-dependent type 2 innate lymphoid cells are required and sufficient for mucous metaplasia in immature mice. Am J Physiol Lung Cell Mol Physiol. 2017;312(6):L983-L993. [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, 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 | 2.4671 mL | 12.3353 mL | 24.6706 mL | 61.6766 mL |
| 5 mM | 0.4934 mL | 2.4671 mL | 4.9341 mL | 12.3353 mL | |
| 10 mM | 0.2467 mL | 1.2335 mL | 2.4671 mL | 6.1677 mL | |
| 15 mM | 0.1645 mL | 0.8224 mL | 1.6447 mL | 4.1118 mL | |
| 20 mM | 0.1234 mL | 0.6168 mL | 1.2335 mL | 3.0838 mL | |
| 25 mM | 0.0987 mL | 0.4934 mL | 0.9868 mL | 2.4671 mL | |
| 30 mM | 0.0822 mL | 0.4112 mL | 0.8224 mL | 2.0559 mL | |
| 40 mM | 0.0617 mL | 0.3084 mL | 0.6168 mL | 1.5419 mL | |
| 50 mM | 0.0493 mL | 0.2467 mL | 0.4934 mL | 1.2335 mL | |
| 60 mM | 0.0411 mL | 0.2056 mL | 0.4112 mL | 1.0279 mL | |
| 80 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7710 mL | |
| 100 mM | 0.0247 mL | 0.1234 mL | 0.2467 mL | 0.6168 mL |
SR3335 Related Classifications
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