JNJ-39758979

JNJ-39758979

• CAS Number: 1046447-90-8
• UNSPSC Description: JNJ-39758979 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].
• Target Antigen: 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 Weight: 221.308
• 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
• Storage Conditions: 4°C (Powder, protect from light)
• Clinical Information: Phase 2