Ipratropium bromide (Sch 1000) 是毒蕈碱的受体 (muscarinic receptor) 的拮抗剂，对 M1、M2 和 M3 受体的结合的IC50值分别为 2.9 nM、2 nM 和 1.7 nM。Ipratropium bromide 具有放松平滑肌的作用，可用于慢性阻塞性肺病 (COPD) 和哮喘等研究。
| 生物活性 | Ipratropium bromide (Sch 1000) is amuscarinic receptorantagonist, withIC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3][4][5]. |
| IC50& Target | 2.9 nM (mAChR M1), 2 nM (mAChR M2), and 1.7 nM (mAChR M3)[3] |
体外研究
(In Vitro) | Ipratropium bromide (1 nM, 10 nM, 100 nM; 15 min) exerts its toxic effects via disruption of mitochondrial membrane potential[1].
Ipratropium bromide (1 nM-1 μM; 4 h) increases infarct size in isolated perfused heart ischaemia/reperfusion experiments with a dose-responsive manner (EC50=22.7 nM)[1].
Ipratropium bromide (0.001 nM-0.1 mM; 2 h) inhibits adult rat cardiac myocyte growth after 4 h hypoxia treatment[1].
Cell Viability Assay[1] | Cell Line: | Adult Rat Cardiac Myocyte | | Concentration: | 0.001 nM-0.1 mM | | Incubation Time: | 2 h in dark; prior to 4 h hypoxia | | Result: | Resulted cell viability in a dose-dependent manner, with the inhibition rate of 52.7% at 0.1 mM dose. |
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体内研究
(In Vivo) | Ipratropium bromide (1.0 μg/kg; i.v.; single dose) enhances vagal nerve stimulation induing bronchoconstriction[2].
Ipratropium bromide (0.04 mg/20 mL and 0.20 mg/20 mL; 30 min, rate=30 mL/30 min) can protect the lungs against the cadmium-induced acute neutrophilic inflammation by reducing the parenchyma inflammatory infiltration of neutrophils[4].
| Animal Model: | Guinea-pigs of the Dunkin Hartley strain[2]. | | Dosage: | 0.1-1 μg/kg | | Administration: | Intravenous injection; single dose | | Result: | Resulted little blocking effect on post-junctional muscarinic receptors at 0.3 μg/kg, and inhibited ACh-induced bronchoconstriction at 0.5 μg/kg. |
| Animal Model: | Male Sprague-Dawley rats (300-350 g)[4] | | Dosage: | 0.04 mg/20 mL and 0.20 mg/20 mL | | Administration: | Inhalation; atomization rate of 30 mL/30 min; 30 min | | Result: | Had no significant effects on any parameters recorded in healthy rats but exerted a protective effect against the inflammatory reaction elicited by cadmium. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(242.51 mM;Need ultrasonic) DMSO : ≥ 35 mg/mL(84.88 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.4251 mL | 12.1253 mL | 24.2507 mL | | 5 mM | 0.4850 mL | 2.4251 mL | 4.8501 mL | | 10 mM | 0.2425 mL | 1.2125 mL | 2.4251 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 50 mg/mL (121.25 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.06 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.06 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.06 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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