MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

JNJ-39758979

CAS No. : 1046447-90-8

MCE 国际站：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 K_i 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。

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 K_i 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 K_i=5.3 nM and the pA2=8.3. At the monkey H₄R, the K_i=25 nM and the pA2=7.5. The affinity for the rat (K_i=188 nM, pA2 = 7.2) and guinea pig H₄R (K_i=306 nM) is moderate, and JNJ 39758979 has little if any affinity for the dog H₄R (K_i≥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 (t_1/2 >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 C_max, t_1/2 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 t_1/2 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  |  Perphenazine-d₈ dihydrochloride  |  Zotepine  |  Emedastine difumarate  |  Cipralisant (enantiomer)  |  Doxepin-d₃ hydrochloride  |  ST-1006  |  Chlorphenoxamine  |  Clemastine-d₅ fumarate  |  H3 receptor-MO-1  |  Izuforant  |  ABT-239  |  Fexofenadine  |  Ketotifen fumarate  |  S 38093  |  Roxatidine  |  Histamine phosphate  |  Ciproxifan maleate  |  LML134  |  Olopatadine-d₃ hydrochloride  |  JNJ10191584 maleate  |  (Z)-Olopatadine-d₃ hydrochloride  |  Cetirizine  |  Cinitapride  |  ICI 162846  |  Diphenylpyraline hydrochloride  |  Doxylamine-d₅  |  Cyclizine lactate  |  FRG8701  |  Methdilazine hydrochloride  |  Azelastine hydrochloride

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

货号: HY-101189

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 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；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   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。