1. NF-κB Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation PI3K/Akt/mTOR
  2. NF-κB Glutathione Peroxidase TNF Receptor Interleukin Related mTOR SOD
  3. Anti-inflammatory agent 107

Anti-inflammatory agent 107 是一种口服有效的抗炎剂。Anti-inflammatory agent 107 能够以 -9.4578 kcal/mol 的优异结合亲和力抑制 NF-κB。Anti-inflammatory agent 107 降低了抗炎因子 (TNF-αIL-6INF-γNF-κβ,CRP (C 反应蛋白) 和 ESR (红细胞沉降率) (Erythrocyte Sedimentation Rate)) 的含量并且提升 SOD (超氧化物歧化酶), CAT (过氧化氢酶) 和 GSH (谷胱甘肽) 的活性来增强内源性抗氧化防御系统。Anti-inflammatory agent 107 无肝肾毒性并且展现出显著的肝肾保护作用。Anti-inflammatory agent 107 能剂量依赖性地改善白细胞浸润和组织水肿。Anti-inflammatory agent 107 可用于抗炎研究。

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Anti-inflammatory agent 107

Anti-inflammatory agent 107 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anti-inflammatory agent 107 is an orally active anti-inflammatory agent. Anti-inflammatory agent 107 inhibits and NF-κB with a superior binding affinity of -9.4578 kcal/mol. Anti-inflammatory agent 107 reduces levels of inflammatory biomarkers (TNF-α, IL-6, INF-γ, NF-κβ, C-reactive protein and Erythrocyte Sedimentation Rate) and enhances the endogenous antioxidant defense system by elevating SOD (Superoxide Dismutase), CAT (Catalase) and GSH (Glutathione) activities. Anti-inflammatory agent 107 not induces liver toxicity and demonstrates hepatoprotective effects. Anti-inflammatory agent 107 dose-dependently ameliorates leukocyte infiltration and tissue edema. Anti-inflammatory agent 107 can be used for anti-inflammatory research[1].

IC50 & Target[1]

NF-κB

 

IL-6

 

mTOR

 

体外研究
(In Vitro)

Anti-inflammatory agent 107 (compound 4D) 通过抑制主要炎症蛋白信号通路 NF-κB (对接评分为 -9.4578 kcal/mol) 发挥强大的抗炎作用[1]
Anti-inflammatory agent 107 (在 2 mL 体系中浓度为 50 μg/mL,在 0.02 mL 体系中浓度为 50 μg/mL) 在人类红细胞膜稳定化 (抗溶血) 实验和蛋白质变性抑制实验中均显示出强效的抗炎活性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Anti-inflammatory agent 107 (compound 4D) (20-50 μg/kg,口服,每日一次,持续一周) 能够降低炎症生物标志物水平,增强并恢复抗氧化防御系统 (GSH、CAT、SOD) 的功能,减轻肾毒性,并减少 κ-Carrageenan (HY-138962) 诱导的足爪水肿大鼠模型中的白细胞浸润[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: κ-Carrageenan (0.1 mL of 1 % W/V, inject into the subplantar region of the right hind paw, once)-induced male (Sprague Dawley) rats (120-125 g, 6-8 weeks)[1].
Dosage: 20, 30 and 50 μg/kg
Administration: p.o., once daily for a week
Result: Showed gradually improvement at different doses.
Showed gradually improvement, gave very close results compare to aspirin at 30 μg/kg.
Reduced levels of inflammatory biomarkers (TNF-α, IL-6, INF-γ, NF-κβ, CRP and ESR) at he high-dose 50 μg/kg.
Showed excellent malondialdehyde (MDA) and nitric oxide (NO) improvement especially at 30 and 50 μg/kg.
Reduced GSH concentrations, returned CAT and SOD activities to nearly normal ranges.
Showed good regression in hepatic enzyme secretion, total bilirubin conjugation and excretion, and albumin biosynthesis.
Reversed the carrageenan-induced renal toxicity (characterized by increased urea and creatinine) and restored these parameters to near-normal ranges.
Produced dose-dependent improvements in histopathology, reducing leukocyte infiltration at lower doses and nearly eliminating edema while restoring normal skin architecture at the highest dose (50 μg/kg).
分子量

628.57

Formula

C29H20N6O9S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Anti-inflammatory agent 107
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HY-179502
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