Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 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.
説明 | JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 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. |
ターゲット&IC50 | H4 receptor:12.5 nM (ki)(in human), H4 receptor:188 nM (ki)(in rat), H4 receptor:25 nM (ki)(in Monkey), H4 receptor:306 nM (ki)(in Guinea pig), H4 receptor:5.3 nM (ki)(in mouse) |
In vitro | JNJ-39758979 is metabolically stable (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes. JNJ 39758979 is a selective and high-affinity histamine H4 receptor antagonist (Ki: 12.5 nM versus the human H4 receptor). In transfected cells, functionally antagonizes histamine-induced cAMP inhibition ( pA2: 7.9). 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 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]. |
In vivo | JNJ-39758979 (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. JNJ-39758979 (10 mg/kg; p.o.) treatment displays that the Cmax, t1/2, and F values are 0.3 μM, 7.5 hours, and 36%, respectively [1]. |
分子量 | 221.3 |
分子式 | C11H19N5 |
CAS No. | 1046447-90-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (135.56 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. 詳細
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JNJ-39758979 1046447-90-8 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor agranulocytosis histamine selective toxicity cAMP inhibit oral anti-inflammatory Inhibitor antipruritic JNJ 39758979 JNJ39758979 inhibitor