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JNJ-39758979 (dihydrochloride)

Products Details

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

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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