SR3335 (Synonyms: ML 176) |
Katalog-Nr.GC12877
One-Click Copy Product Info
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SR3335 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor alpha (RORα), with a Ki value of 220nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 293753-05-6
Sample solution is provided at 25 µL, 10mM.
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SR3335 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor alpha (RORα), with a Ki value of 220nM[1]. RORα is a member of the nuclear receptor superfamily that functions as a transcription factor regulating lipid metabolism, circadian rhythm, immune responses, and cellular differentiation[2]. SR3335 is commonly used in studies on obesity treatment, as well as metabolic disorders, autoimmune diseases, and inflammatory conditions[3,4].
In vitro, SR3335 (20μM) pretreatment for 4h followed by high glucose (33.3mM) stimulation of cardiac fibroblasts for 48h increased the number of 5-ethynyl-2’-deoxyuridine (EdU)-positive cells and elevated the protein expression level of proliferating cell nuclear antigen (PCNA)[5]. SR3335 (2μM) treatment of bone marrow mesenchymal stem cells (BMSCs) for 14 days significantly promoted adipogenic differentiation of BMSCs[6]. SR3335 (1μM) pretreatment of human nucleus pulposus cells for 2h followed by TNF-α (10ng/mL) treatment significantly restored the TNF-α-induced downregulation of Collagen type II (COL2A1) and Aggrecan (ACAN) mRNA expression levels[7].
In vivo, SR3335 (15mg/kg; twice daily) administered via intraperitoneal injection to C57BL/6J mice with laser-induced choroidal neovascularization (CNV) for 8 days (from day 0 to day 7 post-laser) significantly increased CNV lesion area and the proportion of fundus vascular leakage[8].
References:
[1] KUMAR N, KOJETIN D J, SOLT L A, et al. Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist[J]. ACS Chemical Biology, 2011, 6(3): 218-222.
[2] JETTEN A M. Retinoid-related orphan receptors (RORs): critical roles in development, immunity, circadian rhythm, and cellular metabolism[J]. Nuclear Receptor Signaling, 2009, 7(1): nrs.07003.
[3] KAMENECKA T M, LYDA B, CHANG M R, et al. Synthetic modulators of the retinoic acid receptor-related orphan receptors[J]. MedChemComm, 2013, 4(5): 764-776.
[4] AUCLAIR M, ROBLOT N, CAPEL E, et al. Pharmacological modulation of RORα controls fat browning, adaptive thermogenesis, and body weight in mice[J]. American Journal of Physiology-Endocrinology and Metabolism, 2021, 320(2): E219-E233.
[5] SAN W, ZHOU Q, SHEN D, et al. Roles of retinoic acid-related orphan receptor α in high glucose-induced cardiac fibroblasts proliferation[J]. Frontiers in Pharmacology, 2025, 16: 1539690.
[6] HE L, CHEN Z, HE T, et al. Retinoic acid-related orphan nuclear receptor alpha inhibits adipogenic differentiation of bone marrow mesenchymal stem cells via activating WNT/β-catenin signaling pathway[J]. European Journal of Medical Research, 2025, 30(1): 1073.
[7] LIANG T, QIU J, LI S, et al. Inverse Agonist of Retinoid‐Related Orphan Receptor‐Alpha Prevents Apoptosis and Degeneration in Nucleus Pulposus Cells via Upregulation of YAP[J]. Mediators of Inflammation, 2021, 2021(1): 9954909.
[8] LIU C H, YEMANYI F, BORA K, et al. Genetic deficiency and pharmacological modulation of RORα regulate laser-induced choroidal neovascularization[J]. Aging (Albany NY), 2023, 15(1): 37.
| Cell experiment [1]: | |
Cell lines | Cardiac fibroblast |
Preparation Method | Cardiac fibroblasts were pretreated with 20μM SR3335 for 4h and incubated with high glucose (33.3mM) for 48h, then cell proliferation was assessed using EdU staining, and protein expression of PCNA was evaluated by Western blot analysis. |
Reaction Conditions | 20μM; 4h |
Applications | Treatment of SR3335 increased the number of EdU-positive cells and enhanced the protein expression level of PCNA. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice with laser-induced CNV |
Preparation Method | C57BL/6J mice were subjected to laser-induced CNV and treated with SR3335 (15mg/kg; twice daily, i.p.) for 8 days (from day 0 to day 7 post-laser), CNV was analyzed in choroidal flat mounts with isolectin B4 staining to visualize and quantify lesion size. |
Dosage form | 15mg/kg; twice daily; 8 days; i.p. |
Applications | Treatment of SR3335 significantly increases the area of CNV lesions. |
References: | |
| Cas No. | 293753-05-6 | SDF | |
| Überlieferungen | ML 176 | ||
| Chemical Name | N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]thiophene-2-sulfonamide | ||
| Canonical SMILES | C1=CSC(=C1)S(=O)(=O)NC2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O | ||
| Formula | C13H9F6NO3S2 | M.Wt | 405.34 |
| Löslichkeit | ≥ 88.8 mg/mL in DMSO, ≥ 87.4 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4671 mL | 12.3353 mL | 24.6706 mL |
| 5 mM | 493.4 μL | 2.4671 mL | 4.9341 mL |
| 10 mM | 246.7 μL | 1.2335 mL | 2.4671 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)