TNF-α-IN-29
TNF-α-IN-29 is an orally active and selective TNF-α inhibitor, with IC50 values of 123.0 nM against human targets, and a human Kd of 45.9 nM. TNF-α-IN-29 blocks TNF-α-TNFR1 protein-protein interactions and inhibits TNF-α-mediated inflammatory signaling pathways. TNF-α-IN-29 exhibits anti-inflammatory effects in a mouse model of collagen-induced arthritis and promotes articular cartilage repair. TNF-α-IN-29 can be used for the research of rheumatoid arthritis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C29H27ClF3N7O
- 分子量:582.02
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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TNF-α 123 nM (IC50) |
TNF-α 45.9 nM (Kd) |
TNF-α-IN-29 (XS-18) binds strongly to human TNF-α protein with an FP-IC50 of 123.0 nM and a Kd of 45.9 nM, and inhibits the protein-protein interaction between TNF-α and TNFR1 with an IC50 of 36.4 nM.
TNF-α-IN-29 (up to 60 min) has enhanced in vitro metabolic stability in human liver microsomes with a half-life of 63.6 min[1].
TNF-α-IN-29 (1.37-1000 nM; 1.5 h preincubated with TNF-α, 24 h incubated with cells) neutralizes TNF-α-induced apoptosis in L929 cells[1].
TNF-α-IN-29 (20 min preincubated with TNF-α, 18 h incubated with cells) inhibits TNF-α-induced NF-κB activation in NF-κB-TA-Luc HEK293 cells with an IC50 of 126.9 nM and exhibits minimal cytotoxicity at 20 μM[1].
TNF-α-IN-29 (5-10 μM; 72 h incubated with cells, 15 min stimulated with TNF-α) blocks TNF-α-mediated NF-κB pathway activation in MH7A cells by reducing IκBα phosphorylation and suppresses IL-6 mRNA expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L929 cells
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Concentration:1.37, 12, 111, 1000 nM
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Incubation Time:1.5 h (preincubated with TNF-α); 24 h (incubated with cells)
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Result:Inhibited L929 cell apoptosis with a neutralization rate of 68.1% at 1 μM.
Maintained a nearly 50% inhibitory effect at a concentration of 1.37 nM.
TNF-α-IN-29 (5-50 mg/kg; p.o.; twice daily; 14 days) exhibits dose-dependent anti-rheumatoid arthritis activity in the CIA mouse model, with the 50 mg/kg dose demonstrating superior efficacy to Tofacitinib (HY-40354) in reducing joint inflammation, repairing cartilage damage, and inhibiting pro-inflammatory cytokine expression (IL-6 and TNF-α)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/1J (male, 6 weeks old, 16-19 g, collagen-induced arthritis model)[1]
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Dosage:5 mg/kg; 15 mg/kg; 50 mg/kg
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Administration:p.o.; twice daily; 14 days
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Result:Showed dose-dependent inhibition of hind paw volume increase and paw thickening; 15 mg/kg presented efficacy similar to tofacitinib, and 50 mg/kg showed better effects on arthritis scores.
Ameliorated joint histopathological injury dose-dependently; 50 mg/kg markedly reduced inflammatory infiltration and synovial hyperplasia, with stronger effects than tofacitinib.
Improved cartilage repair in a dose-dependent manner; 50 mg/kg significantly restored cartilage structure and exhibited superior efficacy to tofacitinib.
Dose-dependently suppressed IL-6 and TNF-α expression in ankle joints; 15 mg/kg was comparable to tofacitinib, and 50 mg/kg showed stronger inhibition.
化学情報
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分子量 582.02
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分子式 C29H27ClF3N7O
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SMILES
ClC1=C(C2=CC(C3=CN=C(N=C3)N4CCC5(CC4)CN(C5)C(N)=O)=CC=C2N=C1)NC6=CC(C)=CC=C6C(F)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TNF-α-IN-29 関連分類
HY-182884 関連分類
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