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- Tiotropium Bromide hydrate 139404-48-1;411207-31-3

- Tiotropium Bromide hydrate 139404-48-1;411207-31-3
Tiotropium Bromide hydrate 139404-48-1;411207-31-3
产品描述 描述 Tiotropium Bromide hydrate is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.纯度 98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 可溶性/溶解性 DMSO:8 mg/mL (16.31 mM)生物活性 靶点 AChRIn vitro(体外研究) Tiotropium bromide is a potent muscarinic antagonist with equal affinity for M1-, M2- and M3-receptors and is approximately 10-fold more potent than ipratropium bromide. Tiotropium bromide has a potent inhibitory effect against cholinergic nerve-induced contraction of guinea-pig and human airways, that has a slower onset than atropine or ipratropium bromide. Tiotropium bromide, ipratropium bromide and atropine all increase ACh release on neural stimulation and that this effect is washed out equally quickly for the three antagonists. Tiotropium bromide dissociates slowly from M3-receptors (on airway smooth muscle) but rapidly from M2 autoreceptors (on cholinergic nerve terminals). Tiotropium significantly inhibits the release of chemotactic substances by AM, MonoMac6 and A549 cells. Tiotropium bromide inhibits the Th2 cytokine production from PBMCs.In vivo(体内研究) Tiotropium bromide significantly reduces airway inflammation and the Th2 cytokine production in bronchoalveolar lavage fluid (BALF) in both acute and chronic mouse models of asthma. Tiotropium bromide significantly decreases the goblet cell metaplasia, thickness of airway smooth muscle, and airway fibrosis in a mouse model of asthma. Tiotropium bromide reduces the levels of TGF-beta1 in BALF in a chronic model. Tiotropium inhibits the increase in airway smooth muscle mass, myosin expression, and contractility in a guinea pig model of ongoing allergic asthma. Tiotropium abrogates the LPS-induced increase in neutrophils, goblet cells, collagen deposition and muscularised microvessels in a guinea pig model of chronic obstructive pulmonary disease (COPD), but has no effect on emphysema.参考文献 参考文献 研究领域 研究领域 Drug DiscoverySmall Molecule DrugLead Compound DiscoveryTiotropium Bromide hydrate 139404-48-1;411207-31-3温馨提示:本产品仅作科研实验使用,不支持临床等研究
