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| 产品名称 | AChE ↓ ↑ | AChR ↓ ↑ | mAChR ↓ ↑ | nAChR ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Donepezil |
+++
bAChE, IC50: 8.12 nM hAChE, IC50: 11.6 nM |
98% | |||||||||||||||||
| Loganin |
++
AChE, IC50: 3.95 μM |
99%+ | |||||||||||||||||
| topride HCl |
++
AChE, IC50: 2.04 μM |
98% | |||||||||||||||||
| Dehydroevodiamine HCl | ✔ | 99%+ | |||||||||||||||||
| Jatrorrhizine |
++
AChE, IC50: 872 nM |
99%+ | |||||||||||||||||
| Palmatine |
++
AChE, IC50: 0.51 μM |
95% | |||||||||||||||||
| (-)-Huperzine A |
++++
AChE (G4 form), Ki: 7 nM |
98% | |||||||||||||||||
| Galanthamine HBr |
++
AChE, IC50: 0.35 μM |
98% | |||||||||||||||||
| Trospium chloride | ✔ | 99% | |||||||||||||||||
| Tiotropium Bromide Monohydrate | ✔ | 97% | |||||||||||||||||
| Gallamine Triethiodide |
+
AChR, IC50: 68.0 μM |
98% | |||||||||||||||||
| Hexamethonium Bromide | ✔ | 99% | |||||||||||||||||
| Pancuronium dibromide | ✔ | 98% | |||||||||||||||||
| Neostigmine bromide | ✔ | 98% | |||||||||||||||||
| Orphenadrine citrate | ✔ | 98% | |||||||||||||||||
| Oxybutynin | ✔ | 98% | |||||||||||||||||
| Irsogladine | ✔ | PDE | 99% | ||||||||||||||||
| Pyridostigmine bromide | ✔ | 99+% | |||||||||||||||||
| Rivastigmine |
+
AChR, IC50: 5.5 μM |
98% | |||||||||||||||||
| Paroxetine HCl | ✔ | 99% | |||||||||||||||||
| Rocuronium Bromide | ✔ | 98% | |||||||||||||||||
| Tropicamide |
+++
M4 mAChR, IC50: 8 nM |
98% | |||||||||||||||||
| Diphenmanil methylsulfate | ✔ | 97% | |||||||||||||||||
| Umeclidinium bromide | ✔ | 95% | |||||||||||||||||
| Otilonium bromide | ✔ | 98% | |||||||||||||||||
| Flavoxate HCl |
+
mAChR, IC50: 12.2 μM |
99% | |||||||||||||||||
| Ipratropium bromide | ✔ | 98% | |||||||||||||||||
| Diphenidol HCl | ✔ | 98% | |||||||||||||||||
| Darifenacin hydrobromide |
++++
M3 mAChR, pKi: 8.9 |
98% | |||||||||||||||||
| Aclidinium Bromide |
++++
M2 mAChR, Ki: 0.1 nM M4 mAChR, Ki: 0.21 nM |
98% | |||||||||||||||||
| Oxybutynin chloride | ✔ | 99% | |||||||||||||||||
| Pentoxyverine citrate | ✔ | 98% | |||||||||||||||||
| Solifenacin | ✔ | 98% | |||||||||||||||||
| Catharanthine | ✔ | 98% | |||||||||||||||||
| Benzethonium chloride |
+++
α4β2 nAChRs, IC50: 49 nM α7 nAChRs, IC50: 122 nM |
99+% | |||||||||||||||||
| Vinblastine sulfate |
+
nAChR, IC50: 8.9 μM |
99% | |||||||||||||||||
| PNU-120596 |
++
α7 nAChR, EC50: 216 nM |
99+% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Ipratropium Bromide, as short‐acting anticholinergic, is indicated for the maintenance treatment of bronchospasm associated with COPD (chronic obstructive pulmonary disease), including chronic bronchitis and emphysema[3]. Both IB (Ipratropium Bromide) and AS (Albuterol Sulfate) elicit significant bronchodilation, although the magnitude of the bronchodilator response is greater following IB[4]. Moreover, routine nebulized ipratropium bromide premedication for bronchoscopy could be useful and beneficial[5]. |
| Concentration | Treated Time | Description | References | |
| ILC2s | 0.4 mg/ml | 4 h | ACh potently activated ILC2s as measured by intracellular cytokine staining of IL-5 and IL-13. | Sci Immunol. 2021 Mar 5;6(57):eabe3218. |
| human isolated bronchial smooth muscle | 10 nM | 3.0 h | To evaluate the inhibitory effect of ipratropium on human bronchial smooth muscle and its duration. Results showed that the inhibitory effect of ipratropium was short-lasting, with 110% recovery of response after 6 h. | Br J Pharmacol. 2006 Jun;148(3):291-8. |
| guinea-pig isolated tracheal smooth muscle | 10 nM | 0.5 h | To evaluate the inhibitory effect of ipratropium on carbachol-induced contraction and its duration. Results showed that the inhibitory effect of ipratropium was short-lasting, with 70% recovery of response after 4.5 h. | Br J Pharmacol. 2006 Jun;148(3):291-8. |
| Administration | Dosage | Frequency | Description | References | ||
| Guinea pigs | ACh-induced bronchoconstriction in anaesthetized guinea-pig model | Intratracheal instillation | 1.45 nM/kg | Single administration, effects evaluated at 3 and 24 hours | To evaluate the inhibitory effect of ipratropium on ACh-induced bronchoconstriction and its duration. Results showed that the inhibitory effect of ipratropium was short-lasting, with 28.3% inhibition at 3 hours and 14.2% at 24 hours. | Br J Pharmacol. 2006 Jun;148(3):291-8. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03405090 | Chronic Obstructive Pulmonary ... 展开 >>Disease 收起 << | Phase 4 | Recruiting | August 2019 | Canada, Ontario ... 展开 >> Respiratory Investigation Unit Recruiting Kingston, Ontario, Canada, K7L 2V7 Contact: Megha Ibrahim Masthan, MSc 613-549-6666 ext 4314 mim5@queensu.ca Contact: Sandra Vincent 613-549-6666 ext 4890 vincents@queensu.ca Principal Investigator: Denis E O'Donnell, MD, FRCPC 收起 << |
| NCT00498251 | Lung Injury, Acute ... 展开 >> Thoracotomy Anesthesia Intensive Care, Surgical Extravascular Lung Water 收起 << | Not Applicable | Completed | - | Switzerland ... 展开 >> University Hospital of Geneva Geneva, Switzerland, CH-1211 收起 << |
| NCT01395875 | - | Completed | - | - | |
[1]Zhang W, et al. Eur J Pharmacol,?010, 647(1-3), 178-187.
[2]Shaik N, et al. Cell Physiol Biochem,?012, 30(6), 1517-1525.
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.43mL 0.49mL 0.24mL |
12.13mL 2.43mL 1.21mL |
24.25mL 4.85mL 2.43mL |
|
| CAS号 | 22254-24-6 |
| 分子式 | C20H30BrNO3 |
| 分子量 | 412.36 |
| SMILES Code | CC([N@@+]1([C@H]2C[C@@H](C[C@@H]1CC2)OC(C(C3=CC=CC=C3)CO)=O)C)C.[Br-] |
| MDL No. | MFCD00069291 |
| 别名 | Sch 1000; Ipratropium (bromide) |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, room temperature |
| 溶解方案 |
DMSO: 35 mg/mL(84.88 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 100 mg/mL(242.51 mM),配合低频超声助溶 以下溶解方案都请先按照体外实验的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
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