2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. Anti-inflammatory agent 79

Anti-inflammatory agent 79 (compound 17q) 是基于异喹啉酮衍生物的 HIF-1 抑制剂 (IC50: 0.55 μM)，可有效阻断 HIF-1 的信号并增加 HIF-1α 的降解。Anti-inflammatory agent 79 可抑制滑膜的侵袭和迁移，抑制血管生成。Anti-inflammatory agent 79 在小鼠的炎症模型中还有效减轻了足部肿胀和关节炎，下调了体内的炎症因子水平和血管增生。

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Anti-inflammatory agent 79 Chemical Structure

Anti-inflammatory agent 79 Chemical Structure

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Anti-inflammatory agent 79 相关抗体

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查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

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HIF-1α HIF

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body.[13][1].

IC50 & Target

HIF-1α

.55 μM (IC50, [1])

体外研究
(In Vitro)

Anti-inflammatory agent 79 (2.5-10 μM; 24 h) 可浓度依赖性地阻断缺氧诱导的 HIF-1α 蛋白积累，减少炎症反应，抑制细胞侵袭性并促进人 RA 滑膜细胞系中 VHL 依赖性 HIF-1α 降解[1]。

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

Anti-inflammatory agent 79 相关抗体:

Western Blot Analysis[1]

Cell Line: MH7A cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Decreased the protein level of HIF-1α
Decreased the secretion of cytokines, including IL-1β, IL-6 and TNF-α.
体内研究
(In Vivo)

Anti-inflammatory agent 79 (30 mg/kg, 60 mg/kg; ip; 2 天 1 次, 共 16 天) 改善了佐剂诱导关节炎 (AIA) 大鼠模型中踝关节的病理损伤，减少了血管生成并减弱了炎症反应[1]。

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

Animal Model: Adjuvant-induced arthritic (AIA) model in SD rats[1]
Dosage: 30 mg/kg, 60 mg/kg
Administration: ip; once per two days; from 13 to 29 days after CFA injection (vehicle: 5 % ethanol and 5 % cremophor EL in FBS)
Result: Attenuated the development and severity of arthritis
Significantly decreased the HIF-1α expression and the percentage of HIF-1α positive cells.
分子量

315.37

Formula

C21H17NO2
Unlabeled CAS

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

Anti-inflammatory agent 79 相关分类

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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.

Keywords:

Anti-inflammatory agent 79HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHAnti-angiogenesisAnti-inflammationHypoxia-inducible factor 1Isoquinolin-1(2H)-OneRheumatoid arthritisInhibitorinhibitorinhibit

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产品名称：
Anti-inflammatory agent 79
目录号：
HY-163512
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