1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. JNJ-39758979 dihydrochloride

JNJ-39758979 dihydrochloride 

Cat. No.: HY-101189B
Handling Instructions

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.

For research use only. We do not sell to patients.

JNJ-39758979 dihydrochloride Chemical Structure

JNJ-39758979 dihydrochloride Chemical Structure

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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].

IC50 & Target[1]

Human H4 Receptor

12.5 nM (Ki)

Mouse H4 Receptor

5.3 nM (Ki)

Monkey H4 receptor

25 nM (Ki)

Rat H4 receptor

188 nM (Ki)

Guinea pig H4 receptor

306 nM (Ki)

In Vitro

JNJ-39758979 dihydrochloride is a selective, high-affinity histamine H4 receptor antagonist with a Ki 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 Ki=5.3 nM and the pA2=8.3. At the monkey H4R, the Ki=25 nM and the pA2=7.5. The affinity for the rat (Ki=188 nM, pA2 = 7.2) and guinea pig H4R (Ki=306 nM) is moderate, and JNJ-39758979 dihydrochloride has little if any affinity for the dog H4R (Ki≥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 (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes[1].

In Vivo

JNJ-39758979 dihydrochloride (10 mg/kg; p.o.) treatment shows that the Cmax, t1/2 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 t1/2 were 19.9 L/kg, 1.4 μM*h, 2.2 L/h, and 2.1 hours, respectively [1].

Animal Model: Sprague-Dawley rats[1]
Dosage: 10 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: The Cmax, t1/2 and F values were 0.3 μM, 7.5 hours, and 36%, respectively.
Molecular Weight

294.22

Formula

C₁₁H₂₁Cl₂N₅

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

JNJ-39758979JNJ39758979JNJ 39758979Histamine ReceptortoxicityoralhistaminecAMPanti-inflammatoryantipruriticselectiveagranulocytosisInhibitorinhibitorinhibit

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JNJ-39758979 dihydrochloride
Cat. No.:
HY-101189B
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