Ipratropium bromide (Sch 1000) hydrate 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 hydrate 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) hydrate is amuscarinic receptorantagonist, withIC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3][4][5]. |
| IC50& Target | mAChR1 2.9 nM (IC50) | mAChR2 2 nM (IC50) | mAChR3 1.7 nM (IC50) |
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体外研究
(In Vitro) | Ipratropium bromide hydrate (1 nM, 10 nM, 100 nM; 15 min) exerts its toxic effects via disruption of mitochondrial membrane potential[1].
Ipratropium bromide hydrate (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 hydrate (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 hydrate (1.0 μg/kg; i.v.; single dose) enhances vagal nerve stimulation induing bronchoconstriction[2].
Ipratropium bromide hydrate (0.04 mg/20 mL and 0.20 mg/20 mL; inhalation for 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 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: H2O : 62.5 mg/mL(145.22 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.3235 mL | 11.6176 mL | 23.2353 mL | | 5 mM | 0.4647 mL | 2.3235 mL | 4.6471 mL | | 10 mM | 0.2324 mL | 1.1618 mL | 2.3235 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。-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 (116.18 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
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