Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tiotropium Bromide hydrate (BA-679 BR hydrate) 是长效的毒蕈碱受体拮抗剂,可用于治疗慢性阻塞性气道疾病 (COPD)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 266 | 现货 | ||
10 mg | ¥ 378 | 现货 | ||
25 mg | ¥ 622 | 现货 | ||
50 mg | ¥ 913 | 现货 | ||
100 mg | ¥ 1,570 | 现货 | ||
500 mg | ¥ 3,890 | 现货 |
产品描述 | Tiotropium Bromide hydrate (BA-679 BR hydrate) is a potent anticholinergic and bronchodilator, serving as a muscarinic receptor antagonist, specifically targeting mAChR. It is developed for treating chronic obstructive airways disease (COPD), demonstrating novel and long-lasting effects. Binding studies with [3H]tiotropium bromide in human lung reveal its high potency and equivalent affinity for M1-, M2-, and M3-receptors, making it roughly 10 times more effective than ipratropium bromide. It notably inhibits cholinergic nerve-induced contraction of both guinea-pig and human airways more potently than atropine or ipratropium bromide, albeit with a slower onset. Tiotropium bromide uniquely presents slow dissociation from M3-receptors on airway smooth muscle and rapid dissociation from M2 autoreceptors on cholinergic nerve terminals. As a quaternary ammonium derivative, it shows high affinity and special kinetic selectivity towards muscarinic receptors across M1-, M2-, and M3-subtypes, due to its slower dissociation from M1- and M3-receptors compared to M2-receptors. |
体外活性 | 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). [1] Tiotropium significantly inhibits the release of chemotactic substances by AM, MonoMac6 and A549 cells. [2] Tiotropium bromide inhibits the Th2 cytokine production from PBMCs. [3] |
体内活性 | 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. [3] Tiotropium inhibits the increase in airway smooth muscle mass, myosin expression, and contractility in a guinea pig model of ongoing allergic asthma. [4] 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. [5] |
别名 | BA-679 BR hydrate, BA 679BR, 噻托溴铵一水合物 |
分子量 | 490.43 |
分子式 | C19H24BrNO5S2 |
CAS No. | 411207-31-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 8 mg/mL (16.31 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.039 mL | 10.1951 mL | 20.3903 mL | 50.9757 mL |
5 mM | 0.4078 mL | 2.039 mL | 4.0781 mL | 10.1951 mL | |
10 mM | 0.2039 mL | 1.0195 mL | 2.039 mL | 5.0976 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tiotropium Bromide hydrate 411207-31-3 Neuroscience AChR BA-679 BR hydrate BA-679 BR Hydrate Tiotropium Bromide Hydrate BA 679BR 噻托溴铵一水合物 Inhibitor inhibitor inhibit