1. Apoptosis
  2. TNF Receptor
  3. TNF-α-IN-25

TNF-α-IN-25 是一种具有口服活性的 TNF-α 抑制剂。TNF-α-IN-25 在荧光偏振结合实验中的 IC50 为 103 nM,在基于细胞 L929 的实验中 IC50 为 505 nM。TNF-α-IN-25 在葡萄糖-6-磷酸异构酶诱导的关节炎模型中抑制足爪肿胀。TNF-α-IN-25 可用于关节炎研究。

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TNF-α-IN-25

TNF-α-IN-25 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

TNF-α-IN-25 is an orally active TNF-α inhibitor. TNF-α-IN-25 shows Fluorescence Polarization (FP) assay IC50 of 103 nM in FP binding assays and L929 assay IC50 of 505 nM in cell-based assays. TNF-α-IN-25 inhibits paw swelling in the glucose-6-phosphate isomerase (GPI) arthritis model. TNF-α-IN-25 can be used for the study of arthritis[1].

体外研究
(In Vitro)

TNF-α-IN-25 (Compound 10) (< 100 μM, 18 h) 在荧光偏振结合实验中显示 IC50 为 103 nM[1]
TNF-α-IN-25 (< 50 μM) 在基于细胞 L929 的实验中显示 IC50 为 505 nM[1]
TNF-α-IN-25 在 HepG2 人细胞中损害线粒体功能,IC50 值大于 40 μM[1]
TNF-α-IN-25 对 hERG 编码的钾离子通道显示弱至中度抑制,hERG IC50 为 9.2 μM[1]

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

体内研究
(In Vivo)

TNF-α-IN-25 (Compound 10) (0.1-30 mg/kg,口服,每日两次,持续 17 天) 在葡萄糖-6-磷酸异构酶 (GPI)诱导的关节炎模型中显著抑制足爪肿胀[1]

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

Animal Model: Male DBA/J mice were immunized intradermally at the base of the tail with 100 μL of 1:1 (v/v) emulsion containing 300 μg of glucose-6-phosphate isomerase (GPI) and 200 μg of heat inactivated Mycobacterium tuberculosis H37Ra[1]
Dosage: 0.1, 0.3, 1, 3, 10, 30 mg/kg
Administration: p.o. twice daily for 17 days
Result: Inhibited paw swelling AUC with the 30 mg/kg dose achieving comparable efficacy to anti-TNF antibody treatment.
Inhibited paw swelling AUC dose-dependently.
分子量

416.45

Formula

C23H21FN6O

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

TNF-α-IN-25 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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TNF-α-IN-25
目录号:
HY-175250
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