JNJ-39758979

JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity[1][2].

Product Specifications

CAS Number

[1046447-90-8]

UNSPSC

12352005

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/JNJ-39758979.html

Purity

99.71

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

NC1=NC(C(C)C)=CC(N2C[C@H](N)CC2)=N1

Molecular Formula

C11H19N5

Molecular Weight

221.31

References & Citations

[1]Savall BM, et al. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists. J Med Chem. 2014 Mar 27;57 (6) :2429-39.|[2]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.