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CAS No. : 243984-11-4
MCE 国际站:Resatorvid
产品活性:Resatorvid (TAK-242) 是一种选择性的 TLR4 信号传导抑制剂。Resatorvid 抑制 NO,TNF-α 和 IL-6 的产生,其 IC50 值分别为 1.8 nM,1.9 nM,1.3 nM。Resatorvid 下调 TLR4 下游信号分子 MyD88 和 TRIF 的表达。Resatorvid 抑制自噬 (autophagy),并在各种炎症性疾病中起关键作用。
研究领域:Immunology/Inflammation | Apoptosis | Autophagy
作用靶点:Toll-like Receptor (TLR) | TNF Receptor | Interleukin Related | Autophagy
In Vitro: Resatorvid suppresses the production of NO, TNF-α, and IL-6 from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33 nM.
Resatorvid (1-100 nM; 4 hours) inhibits mRNA expression of IL-6 and TNF-α induced by LPS and IFN-γ in RAW264.7 cells.
Resatorvid (1-100 nM; 15 minutes; PBMCs cells) markedly inhibits the LPS-induced phosphorylation of extracellular signal-regulated kinase 1/2 (Erk1/2), p38, and JNK/SAPK as well as degradation of IκBβ at a concentration of 100 nM.
In Vivo: Resatorvid (TAK-242; 3 mg/kg; intraperitoneal injection; for 2 days; male C57BL/6 mice) pretreatment markedly and significantly reverses the LPS-induced body weight loss, TA muscle loss, and muscle strength loss. TAK-242 reverses the LPS-induced shrinkage of muscle fibres and increases the interstitial space. TAK-242 blocks systemic catabolic cytokine release and skeletal muscle proteolysis in LPS-administered mice.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Immunology/Inflammation Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | CNS-Penetrant Compound Library | Autophagy Compound Library | Small Molecule Immuno-Oncology Compound Library | Drug Repurposing Compound Library | Antioxidant Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Pyroptosis Compound Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Rare Diseases Drug Library | Antidepressant Compound Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Pain-Related Compound Library | Mitochondrial Protection Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | C29 | RCGD423 | Relfovetmab | Anti-Mouse TNF alpha Antibody | ODN 1018 | Vunakizumab | TLR7 agonist 5 | Tagraxofusp | Dupilumab | IL-17A modulator-2 | Apremilast | Daclizumab | PNRI-299 | Izokibep | QNZ | AN-3485 | ODN 2088 | Ginsenoside F3 | TLR4/NF-κB/MAPK-IN-1 | Broussonin E | Clerodendrin | Vudalimab | Undecane | Utomilumab | 1,4-Dicaffeoylquinic acid | Asunercept | TLR9-IN-1 | Cetrelimab | Hydrangenol | Mulberroside A
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Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-11109
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