2. Apoptosis
  3. TNF Receptor
  4. 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.

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TNF-α-IN-29

TNF-α-IN-29 Chemical Structure

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TNF-α-IN-29 Related Antibodies

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Description

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[1].

IC50 & Target[1]

TNF-α

123 nM (IC50)

TNF-α

45.9 nM (Kd)

In Vitro

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.

TNF-α-IN-29 Related Antibodies

Apoptosis Analysis[1]

Cell Line: L929 cells
Concentration: 1.37, 12, 111, 1000 nM
Incubation Time: 1.5 h (preincubated with TNF-α); 24 h (incubated with cells)
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.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 MRT0-∞ CL Vd AUC0-∞ F
Rat[1] 2 mg/kg i.v. 598.5 ng/mL 0.9 h 2.8 h 4.7 h 0.6 L/h/kg 2.5 L/kg 3200.5 ng/mL·h /
Rat[1] 20 mg/kg p.o. 1600.0 ng/mL 3.2 h 7.1 h 10.7 h 1.2 L/h/kg 11.6 L/kg 18192.6 ng/mL·h 56.8 %
In Vivo

TNF-α-IN-29 (XS-18) (500-1000 mg/kg in mice; 250-500 mg/kg in rats; oral administration) showed no significant body weight changes compared with the control group in the 7-day acute toxicity test in mice and 14-day subacute toxicity test in rats[1].
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.

Animal Model: DBA/1J (male, 6 weeks old, 16-19 g, collagen-induced arthritis model)[1]
Dosage: 5 mg/kg; 15 mg/kg; 50 mg/kg
Administration: p.o.; twice daily; 14 days
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.
Molecular Weight

582.02

Formula

C29H27ClF3N7O
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TNF-α-IN-29 Related Classifications

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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:

TNF-α-IN-29TNF ReceptorTumor Necrosis Factor ReceptorTNFRrheumatoid arthritisL929 cellsjoint cartilageTNF-αinflammatory signaling pathwayscollagen-induced arthritis mouse modelsNF-κB-TA-Luc HEK293 cellsTNFR1MH7A cellshuman liver microsomesInhibitorinhibitorinhibit

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