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• 产品描述： Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases

• 靶点： TLR4;IL-6:1.3 nM (IC50);TNF-R:1.9 nM (IC50);TNF;TLR;Autophagy;Interleukin

• 体内研究：
  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

• 参考文献：
  1. Ii M, et al. A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signaling. 2. Yamada M, et al. Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate. J Med Chem. 2005 Nov 17;48(23) 3. Yuko Ono, et al. TAK-242, a Specific Inhibitor of Toll-like Receptor 4 Signalling, Prevents Endotoxemia-Induced Skeletal Muscle Wasting in Mice. Sci Rep. 2020 Jan 20;10(1):694.

• 溶解性： DMSO  :  100  mg/mL  (276.38  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.764 ml	13.819 ml	27.638 ml
  5 mM	0.553 ml	2.764 ml	5.528 ml
  10 mM	0.276 ml	1.382 ml	2.764 ml
  50 mM	0.055 ml	0.276 ml	0.553 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

• 6. [IF=2.1] Yijue Liu et al."Sinomenine attenuates bleomycin-induced pulmonary fibrosis, inflammation, and oxidative stress by inhibiting TLR4/NLRP3/TGFβ signaling."INHALATION TOXICOLOGY.10.1080/08958378.2024.2335193

• 5. [IF=5.6] Lijuan Liu et al."Geniposide ameliorates psoriatic skin inflammation by inhibiting the TLR4/MyD88/NF-κB p65 signaling pathway and MMP9."INTERNATIONAL IMMUNOPHARMACOLOGY".2024 May;133:112082

• 4. [IF=7.2] Waimei Si et al."Stigmasterol regulates microglial M1/M2 polarization via the TLR4/NF-κB pathway to alleviate neuropathic pain."PHYTOTHERAPY RESEARCH.2023 Oct;:

• 3. [IF=0.593] Jie Zhang et al."The Anti-Inflammatory Effect of 6% HES 200/0.5 on RAW264.7 Cells Induced by LPS through HMGB1/NF-κB Signaling Pathway."Journal of Hard Tissue Biology

• 2. [IF=3.337] Yunxiang Cao et al.Wilforlide A ameliorates the progression of rheumatoid arthritis by inhibiting M1 macrophage polarization.J Pharmacol Sci. 2021 Nov;:

• 1. [IF=2.055] Jieru Han et al."Preventive effect of dioscin against monosodium urate-mediated gouty arthritis through inhibiting inflammasome NLRP3 and TLR4/NF-κB signaling pathway activation: an in vivo and in vitro study."J Nat Med-Tokyo. 2021 Jan;75(1):37-47

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *