SR1078 (Synonyms: SR 1078;SR-1078) |
Catalog No.GC16392
One-Click Copy Product Info
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SR1078은 시트르산 수용체 관련 고아 수용체(RORs) RORα와 RORγ의 작용제로 IC50 값이 1-3µM이다.
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.
SR1078은 시트르산 수용체 관련 고아 수용체(RORs) RORα와 RORγ의 작용제로 IC50 값이 1-3µM이다. SR1078은 RORα와 RORγ의 리간드 결합 영역에 직접 결합해서 이러한 수용체의 전사 활성을 증가시키고 그 결과 RORα/γ 표적 유전자들의 전사를 자극한다[2, 3]. SR1078은 항염증 작용을 통해 골형성 세포 대사를 조절할 수 있다[4].
체외 실험에서 SR1078(2-10µM)으로 인간 신경 모세포종 SH-SY5Y 세포를 24시간 처리하면 세포에서 A2BP1, CYP19A1, NLGN1 그리고 IPTR1 유전자의 발현을 용량 의존적으로 증가시키고 EC50 범위는 3-5μM이다[5]. SR1078(1, 5µM)으로 HepG2 세포를 처리하면 p53 단백질의 발현을 증가시키고 세포사멸을 유도한다[6].
체내 실험에서 SR1078(20mg/kg)은 대장암세포 이종 이식을 한 쥐에게 복강 주사되고 피하 종양의 성장과 종양 세포의 전이를 현저하게 억제하였다[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.
| 세포 실험 [1]: | |
세포 라인 | SH-SY5Y 세포 |
제조 방법 | SH-SY5Y 세포는 SR1078(2-10µM)으로 처리되었고 24시간 후 세포는 수확되었고 cDNA를 준비해서 양적 PCR로 자폐증 스펙트럼 장애(ASD)-관련 유전자들의 발현을 평가하였습니다. |
반응 조건 | 2-10µM; 24시간 동안 |
응용 분야 | SR1078은 SH-SY5Y 세포에서 ASD 관련 유전자들의 발현을 증가시킵니다. SR1078 처리는 A2BP1, CYP19A1, NLGN1 그리고 IPTR1의 발현을 양에 따라 증가시키고 EC50 범위는 3-5μM입니다. |
| 동물 실험 [2]: | |
동물 모형 | 암컷 무흉선 누드 쥐 |
제조 방법 | 피하 종양 모델을 구축하기 위해 2×10⁶ 대장암(CRC) 세포를 100μL PBS에 소생시킨 후 피하 주사하였습니다. 종양 부피는 3~4일마다 종양량을 측정하고 계산하였습니다. 약물 처치 연구를 위해20mg/kg 아토르바스타틴, 20mg/kg SR1078 또는 조합을 복강 주사(i.p.)로 매일 투여하였습니다. 쥐가 안락사된 후 종양을 절제하고 무게를 측정하였습니다. |
제형 | 20mg/kg; i.p. |
응용 분야 | SR1078은 누드 쥐에서 피하 종양 성장을 현저하게 억제하였습니다. |
References: | |
| Cas No. | 1246525-60-9 | SDF | |
| Synonyms | 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 |
| Solubility | ≥ 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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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.
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Quality Control & SDS
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- Purity: >99.50% 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.)