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Product Description
– 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].
Web ID
– HY-101189B
Shipping
– Room temperature
Applications
– COVID-19-immunoregulation
Molecular Formula
– C11H21Cl2N5
References
– [1]Savall BM, et al. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine Hâ‚„ 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.
Molecular Weight
– 294.22
SMILES
– NC1=NC(C(C)C)=CC(N2C[C@H](N)CC2)=N1.[H]Cl.[H]Cl
Clinical Information
– No Development Reported
Research Area
– Inflammation/Immunology
Solubility
– 10 mM in DMSO
Target
– Histamine Receptor
Isoform
– H4 Receptor
Pathway
– GPCR/G Protein;Immunology/Inflammation;Neuronal Signaling
Product type
– Reference compound
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