JNJ-7777120 | MedChemExpress (MCE)

JNJ-7777120 产品活性：JNJ-7777120是一种强效的和具有选择性的 组胺 H4 受体 拮抗剂 (Ki=4.5 nM)。JNJ-7777120 能有效阻断组胺诱导的小鼠气管肥大细胞从结缔组织向上皮细胞的迁移。JNJ-7777120 还能在小鼠 Zymosan 诱导的腹膜炎模型中显著阻断中性粒细胞的浸润。JNJ-7777120 具有研究抗瘙痒和抗炎的较好潜力。 产品来源： https://www.medchemexpress.cn/JNJ-7777120.html 研究领域：GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation 作用靶点：Histamine Receptor In Vitro: JNJ-7777120 (0, 10, 100, 1000 nM; ~6 h) shows functional antagonism of the human and mouse histamine H4 receptors in SK-N-MC cells.? JNJ-7777120 (10 μM; 10 min) blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells.? JNJ7777120 (30-100 μM; 30 min) inhibits dose-dependently the production of thymus and activation-regulated chemokine/CCL17 and macrophage-derived chemokine/CCL22 from antigen-stimulated BMMC. In Vivo: JNJ-7777120 shows equipotent against the human, mouse, and rat receptors and exhibits at least 1000-fold selectivity over H1, H2, or H3 receptors.? 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 (20 mg/kg; s.c.; single daily for 2 days) blocks the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice.? JNJ-7777120 (10 mg/kg; s.c.; single) significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model. 相关产品：Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Neuronal Signaling Compound Library | Neurotransmitter Receptor Compound Library | Anti-Parkinson's Disease Compound Library | Neurodegenerative Disease-related Compound Library | Anti-Obesity Compound Library | Human Metabolite Library | Coagulation and Anti-coagulation Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Bioactive Compound Library Max | Histamine | Clemastine fumarate | Astemizole | Cimetidine | Terfenadine | Amitriptyline hydrochloride | Loratadine | Mecamylamine hydrochloride | Desloratadine | Diphenhydramine hydrochloride | Doxepin Hydrochloride | Osthole | Famotidine | Fexofenadine hydrochloride | Perphenazine | (S)-(+)-Dimethindene maleate | Promethazine hydrochloride | Ketotifen fumarate | Benztropine mesylate | Ritanserin | Lodoxamide | Mepyramine maleate | Mianserin hydrochloride | Cetirizine dihydrochloride | Chlorpheniramine maleate | Mirtazapine | Ebastine | Azelastine hydrochloride | Meclizine dihydrochloride | Ranitidine hydrochloride 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。

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