UNC2541
Based on 1 publication(s) in Google Scholar
UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC50 of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM). UNC2541 abolishes the analgesic and anti-inflammatory effects of ozone in vivo and in vitro.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.71%
- CAS 番号: 1612782-86-1
- 分子式: C24H34FN7O2
- 分子量:471.57
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 UNC2541
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生物活性
製品説明
IC50 & Target
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Mer |
体外実験
UNC2541 (2.5 μM, 4.5 h) abolishes pro-phagocytic effect of ozone and significantly inhibits the engulfment of
apoptotic neutrophils by bone marrow-derived macrophage (BMDMs)[2].
UNC2541 (2.5 μM) inhibits MerTK and can cancel the effect of ozone on SOCS3 and MMP9 in RAW264.7 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male SPF-grade ICR mice and C57BL/6 mice, weighing 20-22 g and aged 6-8 weeks (anesthetized with sodium pentobarbital and sciatic nerve was ligatured by 4-0 chromic gut sutures to establish chronic constriction injury (CCI) model)[2]
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Dosage:25 μM
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Administration:Pretreatment around the sciatic nerve half an hour in advance.
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Result:Significantly abolished the analgesic effect of ozone in CCI mice.
化学情報
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CAS 番号 1612782-86-1
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性状 Solid
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分子量 471.57
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分子式 C24H34FN7O2
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Color White to off-white
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SMILES
O=C(C(C(NCCCC[C@@H]1N)=N2)=CN=C2NCCCCCCNC1=O)NCC3=CC=C(F)C=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Transl Med
Ozone alleviates MSU-induced acute gout pain via upregulating AMPK/GAS6/MerTK/SOCS3 signaling pathway. [Abstract]2023 Dec 8;21(1):890. PMID: 38066599
溶剤 & 溶解度
体外:
DMSO : 10 mg/mL (21.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
純度とドキュメンテーション
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データシート (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. McIver AL, et al. Discovery of Macrocyclic Pyrimidines as MerTK-Specific Inhibitors. ChemMedChem. 2017 Feb 3;12(3):207-213. [Content Brief]
[2]. Ruan S, et al. Ozone promotes macrophage efferocytosis and alleviates neuropathic pain by activating the AMPK/Gas6-MerTK/SOCS3 signaling pathway. Front Immunol. 2024 Nov 19;15:1455771. [Content Brief]
[3]. Fan W, et al. Ozone alleviates MSU-induced acute gout pain via upregulating AMPK/GAS6/MerTK/SOCS3 signaling pathway. J Transl Med. 2023 Dec 8;21(1):890. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1206 mL | 10.6029 mL | 21.2058 mL | 53.0144 mL |
| 5 mM | 0.4241 mL | 2.1206 mL | 4.2412 mL | 10.6029 mL | |
| 10 mM | 0.2121 mL | 1.0603 mL | 2.1206 mL | 5.3014 mL | |
| 15 mM | 0.1414 mL | 0.7069 mL | 1.4137 mL | 3.5343 mL | |
| 20 mM | 0.1060 mL | 0.5301 mL | 1.0603 mL | 2.6507 mL |