JNJ-39758979 | MedChemExpress (MCE)

JNJ-39758979 产品活性：JNJ-39758979是一种选择性的、具有口服活性的、高亲和力的组胺 H4 受体 (histamine H4 receptor) 拮抗剂，对人，小鼠，猴子的组胺 H4 受体的 Ki 值分别为 12.5、5.3 和 25 nM。JNJ-39758979 对组胺诱导的 cAMP 抑制作用具有拮抗作用，pA2 为 7.9。JNJ-39758979 具有良好的抗炎、止痒作用。 产品来源： https://www.medchemexpress.cn/JNJ-39758979.html 研究领域：GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation 作用靶点：Histamine Receptor In Vitro: JNJ 39758979 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 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. JNJ-39758979 is metabolically stable (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes. In Vivo: JNJ-39758979 (10 mg/kg; p.o.) treatment shows that the Cmax, t1/2 and F values are 0.3 μM, 7.5 hours, and 36%, respectively. 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 . 相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Neuronal Signaling Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Endocrinology Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Neurotransmitter Receptor Compound Library | Anti-Parkinson's Disease Compound Library | Neurodegenerative Disease-related Compound Library | Anti-Obesity Compound Library | Coagulation and Anti-coagulation Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Multi-Target Compound 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 | JNJ-7777120 | Azelastine hydrochloride | Meclizine dihydrochloride 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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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途