SR3335是一种具有高效选择性的维甲酸相关孤儿受体α（RORα）反激动剂，Ki值为220nM。
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.
SR3335是一种具有高效选择性的维甲酸相关孤儿受体α（RORα）反激动剂，Ki值为220nM[1]。RORα是一种核受体超家族成员，作为转录因子，可调节脂质代谢、昼夜节律、免疫反应和细胞分化[2]。SR3335通常用于肥胖症治疗及代谢障碍、自身免疫性疾病和炎症性疾病的研究[3,4]。
在体外，SR3335（20μM）预处理4h后，再用高糖（33.3mM）刺激心脏成纤维细胞48h，增加了5-ethynyl-2’-deoxyuridine（EdU）阳性细胞数量，提升了增殖细胞核抗原（PCNA）的蛋白表达水平[5]。SR3335（2μM）处理骨髓间充质干细胞（BMSC）14天，显著促进了BMSC的脂肪生成分化[6]。SR3335（1μM）预处理人髓核细胞2h，再加入TNF-α（10ng/mL）继续处理，显著恢复了TNF-α诱导的Collagen type II（COL2A1）和Aggrecan（ACAN） mRNA表达水平下降[7]。
在体内，SR3335（15mg/kg; twice daily）通过腹腔注射处理激光诱导脉络膜新生血管（CNV）的C57BL/6J小鼠8天（从激光后第0天至第7天），CNV病变面积显著增大，眼底血管渗漏比例增加[8]。
| 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 | |
| 别名 | ML-176;SR 3335;SR-3335;ML176;ML 176 | ||
| 化学名 | 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 | ||
| 分子式 | C13H9F6NO3S2 | 分子量 | 405.34 |
| 溶解度 | ≥ 88.8 mg/mL in DMSO, ≥ 87.4 mg/mL in EtOH | 储存条件 | Store at -20°C |
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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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