SR3335 (Synonyms: ML 176) |
カタログ番号GC12877
One-Click Copy Product Info
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SR3335はレチノイン酸受容体関連オーファン受容体アルファ（RORα）の非常に有力で、選択的な逆アゴニストであり、Ki値は220nMである。
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はレチノイン酸受容体関連オーファン受容体アルファ（RORα）の非常に有力で、選択的な逆アゴニストであり、Ki値は220nMである[1]。RORαは核受容体スーパーファミリーのメンバーであり、脂質代謝、概日リズム、免疫反応と細胞分化を調節する転写因子として機能する[2]。SR3335は通常、肥満の治療、代謝障害、自己免疫疾患と炎症疾患に関する研究に使われている[3,4]。
In vitro（体外）実験で、SR3335（20μM）で4時間前処理し、その後は高グルコース（33.3mM）で心臓線維芽細胞を48時間刺激したところ、5-ethynyl-2’-deoxyuridine（EdU）陽性細胞の数が増え、増殖細胞核抗原（PCNA）のタンパク質発現レベルが向上した[5]。SR3335（2μM）で骨髄間葉系幹細胞（BMSC）を14日間処理したところ、BMSCの脂肪細胞分化を著しく促進した[6]。SR3335（1μM）でヒト髄核細胞を2時間前処理し、TNF-α（10ng/mL）で処理したところ、Collagen type II（COL2A1）とAggrecan（ACAN）mRNA発現レベルのTNF-αに誘発された下方制御を著しく回復させた[7]。
In vivo（体内）実験で、レーザー誘発性の脈絡膜新生血管（CNV）を持つC57BL/6JマウスにSR3335（15mg/kg；毎日二回）を8日間腹腔内注射した（レーザー照射後の0日目から7日目まで）ところ、CNV病変の面積、眼底血管漏出の割合が著しく増えた[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.
| 細胞実験[1]: | |
細胞株 | 心臓線維芽細胞 |
準備方法 | 心臓線維芽細胞を20μM SR3335で4時間前処理し、高グルコース（33.3mM）で48時間インキュベートし、その後細胞の増殖をEdU染色で評価し、PCNAのタンパク質発現をウエスタンブロット分析で評価した。 |
反応条件 | 20μM；4時間 |
アプリケーション | SR3335の処理は、EdU陽性細胞の数を増やし、PCNAのタンパク質発現レベルを向上させた。 |
| 動物実験 [2]: | |
動物モデル | レーザーに誘発されたCNVを持つC57BL/6J |
準備方法 | C57BL/6Jマウスにレーザー誘発性CNVを投与し、SR3335（15mg/kg；毎日二回、腹腔内注射）で8日間処理し（レーザー後の0日目から7日目まで）、イソレクチンB4染色を行った脈絡膜フラットマウント標本でCNVを解析し、病変のサイズを可視化して定量化した。 |
投与形態 | 15mg/kg；毎日二回；8日間；腹腔内注射 |
アプリケーション | SR3335の処理は、CNV病変の面積を著しく増やす。 |
References: | |
| Cas No. | 293753-05-6 | SDF | |
| 同義語 | 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 |
| 溶解度 | ≥ 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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Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)