SR3335 (Synonyms: ML 176) |
Catalog No.GC12877
One-Click Copy Product Info
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SR3335는 레티노산 수용체 관련 고아 수용체 알파 (RORα)의 고효능 및 선택적 역작용제로 Ki 값은 220nM이다.
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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SR3335는 레티노산 수용체 관련 고아 수용체 알파 (RORα)의 고효능 및 선택적 역작용제로 Ki 값은 220nM이다. RORα는 핵 수용체 초가족의 일원으로 지질 대사, 생체 리듬, 면역 반응 및 세포 분화를 조절하는 전사 인자로 기능한다[2]. SR3335는 비만 치료 및 대사 장애, 자가면역 질환, 염증 상태 연구에 일반적으로 사용된다[3,4].
체외 실험에서 SR3335(20μM)로 4시간 전처리 후 고농도 포도당(33.3mM)으로 심장 섬유아세포를 48시간 자극하면 5-ethynyl-2’-deoxyuridine(EdU) 양성 세포 수가 증가하고 증식 세포 핵 항원(PCNA)의 단백질 발현 수준이 상승하였다[5]. SR3335(2μM)으로 골수 중엽 줄기세포 (BMSCs)를 14일간 처리하면 BMSCs의 지방 형성 분화를 현저하게 촉진하였다[6]. SR3335(1μM)으로 인간 수핵 세포를 2시간 전처리한 후 TNF-α(10ng/mL)로 처리하면 TNF-α에 의해 유도된 콜라겐 II형(COL2A1) 및 아그리칸(ACAN) mRNA 발현 수준의 하향 조절을 현저하게 회복시켰다[7].
체내 실험에서 레이저 유도 맥락막 신생혈관(CNV) C57BL/6J 쥐에게 복강 내 투여로 SR3335 (15mg/kg; 1일 2회)를 8일간(레이저 후 0일부터 7일까지) 투여하면 CNV 병변 면적과 안저 혈관 누출 비율을 현저하게 증가시켰다[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.
| 세포 실험 [1]: | |
세포 라인 | 심장 섬유아세포 |
제조 방법 | 심장 섬유아세포를 20μM SR3335로 4시간 전처리한 후 고농도 포도당(33.3mM)에서 48시간 배양하였습니다. 이후 EdU 염색을 이용해서 세포 증식을 평가하고 단백질 자극법으로 PCNA 단백질 발현을 평가하였습니다. |
반응 조건 | 20μM; 4 시간 동안 |
응용 분야 | SR3335 처리는 EdU 양성 세포 수를 증가시키고 PCNA 단백질 발현 수준을 강화하였습니다. |
| 동물 실험 [2]: | |
동물 모형 | C57BL/6J 쥐에 레이저 유도 CNV |
제조 방법 | C57BL/6J 쥐에게 레이저 유도 CNV를 시술하고 SR3335 (15mg/kg; 1일 2회, 복강 내 투여)를 8일간 (레이저 후 0일부터 7일까지) 처리하였습니다. 맥락막 평평한 장착물에서 아이소렉틴 B4 염색을 사용해서 CNV를 분석하고 병변 크기를 시각화 및 정량화하였습니다. |
제형 | 15mg/kg; 매일 2번; 8 일 동안; i.p. |
응용 분야 | SR3335 처리는 CNV 병변 면적을 현저하게 증가시켰습니다. |
References: | |
| Cas No. | 293753-05-6 | SDF | |
| Synonyms | 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 |
| Solubility | ≥ 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 | |||
|
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 in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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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.)