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TNF-α-IN-2

Catalog No. T36097 CAS 2074702-04-6

TNF-α-IN-2 is a highly potent and orally bioavailable inhibitor of tumor necrosis factor alpha (TNFα), exhibiting an IC50 of 25 nM in the HTRF assay. It exerts its inhibitory effects by inducing conformational changes in the TNFα trimer upon binding, resulting in disrupted signaling when the trimer interacts with TNFR1. TNF-α-IN-2 holds promise as a valuable tool for investigating the pathogenesis of rheumatoid arthritis[1].

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TNF-α-IN-2, CAS 2074702-04-6

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 2,450.00
50 mg	10-14 weeks	$ 3,190.00
100 mg	10-14 weeks	$ 5,140.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	TNF-α-IN-2 is a highly potent and orally bioavailable inhibitor of tumor necrosis factor alpha (TNFα), exhibiting an IC50 of 25 nM in the HTRF assay. It exerts its inhibitory effects by inducing conformational changes in the TNFα trimer upon binding, resulting in disrupted signaling when the trimer interacts with TNFR1. TNF-α-IN-2 holds promise as a valuable tool for investigating the pathogenesis of rheumatoid arthritis[1].
Targets&IC50	TNF-α:25 nM (IC50)
In vitro	TNF-α-IN-2 (compound 42), when administered for 30 minutes, effectively suppresses soluble TNFα-induced E-selectin expression in HUVECs, demonstrating an inhibitory concentration (IC50) of 30 nM[1].
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].

Molecular Weight	494.92
Formula	C25H21ClF2N6O
CAS No.	2074702-04-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Xiao HY, et, al. Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches. J Med Chem. 2020 Dec 1.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TNF-α-IN-2 2074702-04-6 TNF-alpha-IN-2 TNF α IN 2 TNFαIN2 TNF-a-IN-2 inhibitor inhibit

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