JNJ-39758979

JNJ-39758979 is a histamine H₄ receptor antagonist (K_i = 12.5 nM for the human receptor).¹ It is selective for the histamine H₄ receptor over histamine H₁, H₂, and H₃ receptors (K_is = >1,000, >1,000, and 1,043 nM, respectively, for the human receptors), as well as 48 other receptors, ion channels, and transporters at 1 µM and 66 kinases at 10 µM. JNJ-39758979 inhibits chemotaxis induced by histamine (Item No. 33828) in isolated mouse bone marrow-derived mast cells (IC₅₀ = 8 nM). It reduces ovalbumin-induced eosinophil infiltration in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of asthma when administered at doses ranging from 0.2 to 20 mg/kg. JNJ-39758979 (20 mg/kg) decreases ear edema in a mouse model of Th2-dependent contact hypersensitivity induced by fluorescein isothiocyanate (FITC; Item No. 33264) and inhibits histamine-induced pruritis in mice.^1,2 It also reduces nephropathy, but does not affect body weight or blood glucose levels, in a mouse model of streptozotocin-induced diabetes when administered at a dose of 100 mg/kg.³

WARNING This product is not for human or veterinary use.

1. Thurmond, R.L., Chen, B., Dunford, P.J., et al. Clinical and preclinical characterization of the histamine H4 receptor antagonist JNJ-39758979. Clinical Trial 349(2), 176-184 (2014).

2. Savall, B.M., Chavez, F., Tays, K., et al. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists. J. Med. Chem. 57(6), 2429-2439 (2014).

3. Pini, A., Grange, C., Veglia, E., et al. Histamine H4 receptor antagonism prevents the progression of diabetic nephropathy in male DBA2/J mice. Pharmacol. Res. 128, 18-28 (2018).