TNF-α-IN-25
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.
For research use only. We do not sell to patients.
- Formula: C23H21FN6O
- Molecular Weight:416.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
TNF-α-IN-25 (Compound 10) (< 100 μM, 18 h) shows Fluorescence Polarization (FP) assay IC50 of 103 nM in the FP binding[1].
TNF-α-IN-25 (< 50 μM) shows L929 assay IC50 of 505 nM in cell-based assays[1].
TNF-α-IN-25 impairs the mitochondrial in HepG2 human cells, with an IC50 value greater than 40 μM[1].
TNF-α-IN-25 demonstrates weak to the moderate inhibition of the potassium ion channel encoded by hERG, with a hERG IC50 of 9.2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:0.1, 0.3, 1, 3, 10, 30 mg/kg
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Administration:p.o. twice daily for 17 days
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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.
Chemical Information
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Molecular Weight 416.45
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Formula C23H21FN6O
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SMILES
CC(O)(C1=NC=C(C=N1)C2=CC=C3N=C4CN5CC6=C([C@H](N4C3=N2)C5)C(F)=CC=C6)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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