JNJ-39758979 Inhibitor

JNJ-39758979 is a selective and high-affinity histamine H receptor antagonist (Kis: 12.5, 5.3, and 25nM for human, mouse, and monkey histamine H receptor, respectively). JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells.

Savall BM, et al. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine Hreceptor antagonists. J Med Chem. 2014 Mar 27;57(6):2429-39.
Savall BM, et al. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H receptor antagonists. J Med Chem. 2014 Mar 27;57(6):2429-39.
Murata Y, et al. Phase 2a, randomized, double-blind, placebo-controlled, multicenter, parallel-group study of a H4 R-antagonist (JNJ-39758979) in Japanese adults with moderate atopic dermatitis.
Murata Y, et al. Phase 2a, randomized, double-blind, placebo-controlled, multicenter, parallel-group study of a H4 R-antagonist (JNJ-39758979) in Japanese adults with moderate atopic dermatitis.

Small volumes of JNJ-39758979, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5753352 is an inhibitor targeting JNJ-39758979.