TNF-α-IN-2 MedChemExpress (MCE)

Product Name	Benzonitrile, 3-[(1R)-1-[[3-chloro-7-fluoro-6-[2-(1-hydroxy-1-methylethyl)-5-pyrimidinyl]-2-methyl-1,5-naphthyridin-4-yl]amino]ethyl]-4-fluoro-
Synonyms	TNF-α-IN-2;Benzonitrile, 3-[(1R)-1-[[3-chloro-7-fluoro-6-[2-(1-hydroxy-1-methylethyl)-5-pyrimidinyl]-2-methyl-1,5-naphthyridin-4-yl]amino]ethyl]-4-fluoro-
CAS	2074702-04-6
EINECS
Chemical Formula	C25 H21 Cl F2 N6 O
Molecular Weight	494.92
inchi
Package	1 mg
Price	Email to quote
Descriptions	TNF-α-IN-2 TNF-α-IN-2 MedChemExpress (MCE) HY-134471 2074702-04-6 98.75% Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Room temperature in continental US Descriptions TNF-α-IN-2 TNF-α-IN-2 MedChemExpress (MCE) HY-134471 2074702-04-6 98.75% Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Room temperature in continental US may vary elsewhere. 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. 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]. 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]. CD40 25 nM (IC50) \| \| \| \| \| \| \| \| \| \| [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. [Content Brief]
Last Update	2025-04-01 14:45:47

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