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

TNF-α-IN-2 

Cat. No.: HY-134471
Handling Instructions

TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis.

For research use only. We do not sell to patients.

TNF-α-IN-2 Chemical Structure

TNF-α-IN-2 Chemical Structure

CAS No. : 2074702-04-6

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Description

TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis[1].

IC50 & Target[1]

TNFα

25 nM (IC50)

In Vitro

TNF-α-IN-2 (compound 42) (30 min) inhibits the E-selectin expression induced by soluble TNFα in HUVECs, with an IC50 of 30 nM[1].

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

In Vivo

TNF-α-IN-2 (5-25 mg/kg; p.o. 1 h before TNF stimulation) inhibits TNF-induced IL-6 in mice[1].
TNF-α-IN-2 (2-10 mg/kg; p.o. twice daily for 10 d) dose dependently reduces both the clinical score as well as the levels of inflammatory cytokines and leukocyte cell surface receptors in mice[1].
TNF-α-IN-2 (0.5 mg/kg; i.v.) exhibits long t1/2 (6.2 h), low CL (6.6 mL/min•kg), and Vss (3.2 L/kg) in mice[1].
TNF-α-IN-2 (2 mg/kg; p.o.) exhibits good oral bioavailability (58%), Cmax (0.47 μM), and AUCtot (5.9 μM•h) in mice[1].

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

Animal Model: Female C57Bl/6 mice[1]
Dosage: 5, 25 mg/kg
Administration: P.o. 1 h prior to TNF stimulation
Result: Inhibited IL-6 moderately at 5 mg/kg while the inhibition at 25 mg/kg was similar to mouse Enbrel, which served as the positive control in the study.
Molecular Weight

494.92

Formula

C₂₅H₂₁ClF₂N₆O

CAS No.

2074702-04-6

SMILES

C[[email protected]](C1=CC(C#N)=CC=C1F)NC2=C(C(C)=NC3=CC(F)=C(C4=CN=C(C(C)(O)C)N=C4)N=C23)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TNF-α-IN-2TNF ReceptorTumor Necrosis Factor ReceptorTNFRtumornecrosisfactorTNFαHTRFrheumatoidarthritisInhibitorinhibitorinhibit

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TNF-α-IN-2
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