HY-078020 | MedChemExpress (MCE)

HY-078020 产品活性：HY-078020 (compound III-4) 是一种具有选择性的，口服有效的 histamine H1 受体拮抗剂 (H1R)， IC50 值为 24.12 nM。HY-078020 在过敏性疾病中具有抗炎作用。 产品来源： https://www.medchemexpress.cn/hy-078020.html 研究领域：GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation 作用靶点：Histamine Receptor | mAChR In Vitro: HY-078020 reveals a potent inhibitory activity towards H1R (IC50 is 24.12 nM) and weak inhibition against M3R and hERG, with IC50s of >10 and 17.6 μM, respectively. HY-078020 exhibits moderate permeability (efflux ratio rate HY-078020 exhibits inhibitory activity against cytochrome P450 (CYP) isozymes CYP3A4 of rates. In Vivo: HY-078020 (5 mg/kg, i.g.) inhibits the histamine induced skin vasodilation and capillary permeability in ICR/KM mice, with a vascular permeability inhibition rates of 58.71 %. HY-078020 (10 mg/kg, i.v.) exhibits aweak anticholinergic activity with an inhibition rate of salivary secretion of 10.8% in Wistar mice. HY-078020 reveals a pharmacokinetic profils in mice: Pharmacokinetic Analysis of HY-078020 in wistar male rats route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-inf (ng·h/mL) Vd (L/kg) CL (mL/h/kg) MRT0-inf(h) F (%) iv 4 0.653 ± 0.12 - - 1678 ± 152.59 1822.38 ± 224.97 1.77 ± 0.22 37.00 ± 4.62 0.70 ± 0.14 59.55 po 25 4.05 ± 0.81 0.38 ± 0.16 1722.06 ± 337.11 6246.92 ± 1443.28 7209.70 ± 1419.01 21.26 ± 7.42 59.35 ± 10.59 6.01 ± 1.42 - 相关产品：Clozapine N-oxide | Deschloroclozapine | Pilocarpine Hydrochloride | Histamine | Atropine | Clemastine fumarate | Scopolamine hydrobromide | Carbamoylcholine chloride | Olanzapine | Astemizole | Cimetidine | Terfenadine | Amitriptyline hydrochloride | Loratadine | Methacholine chloride | Xanomeline | Mecamylamine hydrochloride | Mepenzolate bromide | Desloratadine | Diphenhydramine hydrochloride | Doxepin Hydrochloride | Osthole | Famotidine | Fexofenadine hydrochloride | Perphenazine 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