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。

Umeclidinium bromide

CAS No. : 869113-09-7

MCE 站：Umeclidinium bromide

产品活性：Umeclidinium bromide 是一种 mAChR 拮抗剂。Umeclidinium bromide 作用于克隆的人 M1-M5 mAChRs，K_i 为 0.05 到 0.16 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mAChR

In Vitro: In human embryonic kidney 293 cells, Umeclidinium bromide (GSK573719A) inhibits the human ether-a-go-go-related gene channel tail current in a concentration-dependent manner (IC₅₀=9.4 μM). Umeclidinium bromide, previously known as GSK573719, is a novel high-affinity specific mAChR antagonist. It is a potent agent that demonstrates slow functional reversibility at cloned human M₃ mAChRs and at endogenous mAChR in isolated human bronchus.

In Vivo: When Umeclidinium bromide (GSK573719A) is given once daily to mice for 5 consecutive days (0.025 μg intranasally), the level of inhibition on the fifth day is modestly increased above that obtained after a single administration to the same mice (60 versus 35%, respectively). After the fifth day of dosing, the mice are rested for 5 additional days, allowing bronchomotor tone to return to baseline levels. On the sixth day, the mice receive one last dose of antagonist and are once again challenged with Mch. The level of inhibition is essentially the same as that found on the first day of testing, indicating that tolerance is not evident with repeated intranasal delivery of Umeclidinium bromide. By contrast, when Umeclidinium bromide is given orally (2.0 mg/kg) to mice at a dose 100 times the ED₅₀ value (intranasal), there is no observable protection against an Mch challenge.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Neuronal Signaling Compound Library  |  FDA-Approved Drug Library  |  Drug Repurposing Compound Library  |  NMPA-Approved Drug Library  |  Orally Active Compound Library  |  Neurotransmitter Receptor Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Clozapine N-oxide  |  Deschloroclozapine  |  Pilocarpine Hydrochloride  |  Atropine  |  Olanzapine  |  Amitriptyline hydrochloride  |  Levetiracetam  |  Carbamoylcholine chloride  |  Darifenacin hydrobromide  |  Methacholine chloride  |  Otilonium bromide  |  DREADD agonist 21  |  Peimisine  |  Propantheline bromide  |  Cevimeline hydrochloride hemihydrate  |  Dronedarone  |  L-Hyoscyamine  |  Tiotropium Bromide  |  Xanomeline oxalate  |  Anethole trithione  |  Metixene hydrochloride hydrate  |  Trospium chloride  |  Bethanechol chloride  |  Biperiden Hydrochloride  |  Pirenzepine dihydrochloride  |  Diphenidol hydrochloride  |  Ipratropium bromide

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*新*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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。