JNJ-39758979 dihydrochloride 

JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H₄ receptor antagonist, with K_is 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].

JNJ-39758979 dihydrochloride is a selective, high-affinity histamine H₄ receptor antagonist with a K_i of 12.5 nM versus the human H₄ receptor and functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. At the mouse H₄R, the K_i=5.3 nM and the pA2=8.3. At the monkey H₄R, the K_i=25 nM and the pA2=7.5. The affinity for the rat (K_i=188 nM, pA2 = 7.2) and guinea pig H₄R (K_i=306 nM) is moderate, and JNJ-39758979 dihydrochloride has little if any affinity for the dog H₄R (K_i≥10 μM). The compound is highly selective for H₄R, as it exhibits low affinity for the H₁, H₂, and H₃ receptors^[1].
JNJ-39758979 dihydrochloride is metabolically stable (t_1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-39758979 dihydrochloride (10 mg/kg; p.o.) treatment shows that the C_max, t_1/2 and F values are 0.3 μM, 7.5 hours, 36%, respectively^[1].
JNJ-39758979 dihydrochloride (2 mg/kg; i.v.) treatment shows that the Vss, AUC, CL and t_1/2 were 19.9 L/kg, 1.4 μM*h, 2.2 L/h, and 2.1 hours, respectively ^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

294.22

C₁₁H₂₁Cl₂N₅

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]