SR1078 (Synonyms: SR 1078;SR-1078) |
カタログ番号GC16392
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SR1078はレチノイン酸受容体関連のオーファン受容体(RORs)RORαとRORγの作動剤であり、IC50値は1-3µMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1246525-60-9
Sample solution is provided at 25 µL, 10mM.
SR1078はレチノイン酸受容体関連のオーファン受容体(RORs)RORαとRORγの作動剤であり、IC50値は1-3µMである[1]。SR1078はRORαとRORγのリガンド結合ドメインを直接結合でき、これらの受容体の転写活性を増やし、よってRORα/γ標的遺伝子の転写を刺激する[2, 3]。SR1078は抗炎症作用を通じて、骨芽細胞の代謝を調節できる[4]。
体外で、ヒト神経芽細胞腫SH-SY5Y細胞をSR1078 (2-10µM)で24時間処理した結果、細胞におけるA2BP1、CYP19A1、NLGN1とIPTR1遺伝子の発見を用量依存的に増やし、EC50の範囲は3-5μMである[5]。SR1078 (1、5µM)でHepG2細胞を処理し、p53タンパク質の発見を増やし、細胞のアポトーシスを誘発した[6]。
体内で、大腸癌細胞異種移植を持つマウスに、SR1078 (20mg/kg)を腹腔内注射した結果、皮下腫瘍の成長と腫瘍細胞の転移を著しく阻害した[7]。
References:
[1] Wang Y, Kumar N, Nuhant P, et al. Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ[J]. ACS chemical biology, 2010, 5(11): 1029-1034.
[2] 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.
[3] Nematisouldaragh D, Kirshenbaum E, Uzonna M, et al. The Role of Retinoic-Acid-Related Orphan Receptor (RORs) in Cellular Homeostasis[J]. International Journal of Molecular Sciences, 2024, 25(21): 11340.
[4] Fernandes J, Benderdor M, Shi Q. SR1078, A synthetic ligand of nuclear receptor ror alpha, modulates osteoblast metabolism with anti-inflammatory effects[J]. Osteoarthritis and Cartilage, 2012, 20: S115-S116.
[5] Wang Y, Billon C, Walker J K, et al. Therapeutic effect of a synthetic RORα/γ agonist in an animal model of autism[J]. ACS Chemical Neuroscience, 2016, 7(2): 143-148.
[6] Wang Y, Solt L A, Kojetin D J, et al. Regulation of p53 stability and apoptosis by a ROR agonist[J]. PloS one, 2012, 7(4): e34921.
[7] Wang Y N, Ruan D Y, Wang Z X, et al. Targeting the cholesterol-RORα/γ axis inhibits colorectal cancer progression through degrading c-myc[J]. Oncogene, 2022, 41(49): 5266-5278.
| 細胞実験[1]: | |
細胞株 | SH-SY5Y細胞 |
準備方法 | SH-SY5YをSR1078 (2-10µM)で処理し、24時間後、細胞を採取し、cDNAを準備し、定量PCRで自閉症スペクトラム傷害（ASD）関連の遺伝子の発見を評価した。 |
反応条件 | 2-10µM; 24h |
アプリケーション | SH-SY5Y細胞で、SR1078はASD関連の遺伝子の発見を増やした。SR1078の処理は、A2BP1、CYP19A1、NLGN1とIPTR1の発見を用量依存的に増やし、EC50の範囲は3-5μMである。 |
| 動物実験 [2]: | |
動物モデル | 雌のBALB/c無胸腺ヌードマウス |
準備方法 | 皮下腫瘍モデルを作成するために、2×106個のCRC細胞を100μLのPBSで懸濁し、その後皮下注射した。腫瘍の体積をノギスで3または4日ごとに測定し算出した。薬剤処理の研究について、毎日の用量が20mg/kgのアトルバスタチン、20mg/kg SR1078または併用を腹腔内（i.p.）注射した。マウスを安楽死させた後、腫瘍を切除し、重量を測った。 |
投与形態 | 20mg/kg；腹腔内注射 |
アプリケーション | SR1078は、皮下投与のヌードマウスの腫瘍成長を著しく阻害した。 |
References: | |
| Cas No. | 1246525-60-9 | SDF | |
| 同義語 | SR 1078;SR-1078 | ||
| Chemical Name | N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-4-(trifluoromethyl)benzamide | ||
| Canonical SMILES | C1=CC(=CC=C1C(=O)NC2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O)C(F)(F)F | ||
| Formula | C17H10F9NO2 | M.Wt | 431.25 |
| 溶解度 | ≥ 43.2 mg/mL in DMSO, ≥ 43.4 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 | 2.3188 mL | 11.5942 mL | 23.1884 mL |
| 5 mM | 463.8 μL | 2.3188 mL | 4.6377 mL |
| 10 mM | 231.9 μL | 1.1594 mL | 2.3188 mL |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)