JNJ-7777120

JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.

目録号S2905
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JNJ-7777120 化学構造
分子量: 277.75

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製品の説明

生物活性

情報 JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
目標 Histamine H4 receptor
IC50 4.5 nM (Ki) [1]
In vitro試験 JNJ 7777120 binds with high affinity to the H4 receptor and has a greater than 1000-fold selectivity over the other histamine receptors. JNJ 7777120 is a selective and potent H4 receptor antagonist with little or no affinity for over 50 other targets. [2]
In vivo試験 JNJ 7777120 has an oral bioavailability of ~30% in rats and 100% in dogs, with a half-life of ∼3 h in both species. JNJ 7777120 blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. JNJ 7777120 can block the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice. JNJ 7777120 significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model. [2]
臨床試験
特集

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [1]

Binding assay Cell pellets from SK-N-MC cells transfected with human, rat, or mouse H4 receptor, human H3 receptor, or human H1 receptor are used. For the mouse H1 receptor binding, fresh mouse brain is used. Cell pellets or mouse brain are homogenized in 50 mM Tris pH 7.5 containing 5 mM EDTA, and supernatants from an 800g spin are collected and recentrifuged at 30,000g for 30 min. Pellets are rehomogenized in 50 mM Tris pH 7.5 containing 5 mM EDTA. For the H4 competition binding studies, human, mouse, and rat cell membranes are incubated with 10, 40, and 150 nM [3H]histamine (specific activity 23 Ci/mmol), respectively, with or without JNJ 7777120 for 45 min at 25°C. Nonspecific binding is defined using 100 μM unlabeled histamine. The Kd values for the human, mouse, and rat H4 receptor are determined to be 5, 42, and 178 nM, respectively, and the Bmax values are determined to be 1.12, 1.7, and 0.68 pmol/mg protein, respectively. Similarly, the ligand used for the H3receptor-binding assays is [3H]N-α-methyl histamine (specific activity, 82 Ci/mmol), and the nonspecific binding is defined using 100 μM unlabeled histamine. The Kd values for the human and rat H3 receptor are determined to be 1 and 0.8 nM, respectively, and the Bmax values are 2.13 and 0.4 pmol/mg protein, respectively. The ligand used for the human and mouse H1 receptor binding is [3H]pyrilamine (specific activity, 20 Ci/mmol), and the nonspecific binding is defined using 10 μM unlabeled diphenhydramine. The Kd is 1 nM for human receptor and 3 nM for the mouse receptor. The Bmax is 2.68 pmol/mg protein for the human receptor and 0.2 pmol/mg protein for the mouse receptor. The binding to the guinea pig H1 and H2 receptors is determined by Cerep, Inc. For the H1 receptor-binding assays, guinea pig cerebellum is used. The radioligand is [3H]pyrilamine, and 100 μM triprolidine is used to determine the nonspecific binding. For the H2 receptor-binding assays, guinea pig striatum is used. The radioligand is [3H]aspartate amino-transferase, and 100 μM tiotidine is used to determine the nonspecific binding. The Kd of [3H]JNJ 7777120 (specific activity, 84 Ci/mmol) for the human and mouse H4 receptor is determined essentially as described above using increasing concentrations of [3H]JNJ 7777120 instead of [3H]histamine in the presence of 100 μM unlabeled histamine. For all studies, the Ki values are calculated based on an experimentally determined appropriate Kd value.

動物実験: [2]

動物モデル Female BALB/c mice
製剤 5% (w/v) dextrose in water
投薬量 200 mg/kg
管理 P.O.
1

参考

化学情報

Download JNJ-7777120 SDF
分子量 277.75
化学式

C14H16ClN3O

CAS No. 459168-41-3
別名 JNJ 7777120
溶解度 (25°C)
  • DMSO 56 mg/mL
  • 水 <1 mg/mL
  • エタノール 8 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 Methanone, (5-chloro-1H-indol-2-yl)(4-methyl-1-piperazinyl)-

研究分野

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