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JNJ-39758979 (dihydrochloride)

JNJ-39758979 dihydrochloride 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 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity[1][2].

Product Specifications

UNSPSC

12352005

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/jnj-39758979-dihydrochloride.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C11H21Cl2N5

Molecular Weight

294.22

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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

H4 Receptor

Frequently Asked Questions

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