MONNA
(Synonyms: 2-(4-甲氧基萘-2-基氨基)-5-硝基苯甲酸) 目录号 : GC18358
MONNA是ANO1（anoctamin-1/TMEM16A）钙激活氯通道的特异性阻断剂，对非洲爪蟾卵母细胞中xANO1的IC50为0.08μM。
Cas No.:1572936-83-4
Sample solution is provided at 25 µL, 10mM.
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MONNA is a specific blocker of ANO1 (anoctamin-1/TMEM16A) calcium-activated chloride channels, with an IC50 of 0.08μM for xANO1 in Xenopus laevis oocytes[1]. MONNA modulates epithelial chloride transport and smooth muscle contraction by selectively blocking ANO1-mediated chloride currents[2]. MONNA is commonly used in research on diseases such as hypertension, cystic fibrosis, bronchitis, asthma, and hyperalgesia[3][4].
In vitro, MONNA (1μM; 30s) caused reproducible elevations in intracellular Ca2+ concentration in isolated mouse bronchial smooth muscle cells[5].
In vivo, MONNA (1μM; 30min perfusion) reversed the U46619-induced decrease in coronary flow in Langendorff-perfused rat hearts[6]. MONNA (10μg/day; 3 days; starting on day 4 after SNL; intrathecal injection) reduced SNL-induced up-regulation of anoctamin-1, ATF-3, and caspase-3 protein expression in injured L5 dorsal root ganglia of rats[7].
References:
[1] Oh SJ, Hwang SJ, Jung J, et al. MONNA, a potent and selective blocker for transmembrane protein with unknown function 16/anoctamin-1. Mol Pharmacol. 2013;84(5):726-735.
[2] Liu Y, Liu Z, Wang K. The Ca2+-activated chloride channel ANO1/TMEM16A: An emerging therapeutic target for epithelium-originated diseases?. Acta Pharm Sin B. 2021;11(6):1412-1433.
[3] Galietta LJV. TMEM16A (ANO1) as a therapeutic target in cystic fibrosis. Curr Opin Pharmacol. 2022;64:102206.
[4] Boedtkjer DM, Kim S, Jensen AB, Matchkov VM, Andersson KE. New selective inhibitors of calcium-activated chloride channels - T16A(inh) -A01, CaCC(inh) -A01 and MONNA - what do they inhibit?. Br J Pharmacol. 2015;172(16):4158-4172.
[5] Dwivedi R, Drumm BT, Alkawadri T, et al. The TMEM16A blockers benzbromarone and MONNA cause intracellular Ca2+-release in mouse bronchial smooth muscle cells. Eur J Pharmacol. 2023;947:175677.
[6] Askew Page HR, Dalsgaard T, Baldwin SN, et al. TMEM16A is implicated in the regulation of coronary flow and is altered in hypertension. Br J Pharmacol. 2019;176(11):1635-1648.
[7] García G, Martínez-Rojas VA, Oviedo N, Murbartián J. Blockade of anoctamin-1 in injured and uninjured nerves reduces neuropathic pain. Brain Res. 2018;1696:38-48.
MONNA是ANO1（anoctamin-1/TMEM16A）钙激活氯通道的特异性阻断剂，对非洲爪蟾卵母细胞中xANO1的IC50为0.08μM[1]。MONNA通过选择性阻断ANO1介导的氯离子电流，在上皮氯离子运输和平滑肌收缩中发挥作用[2]。MONNA通常用于高血压、囊性纤维化、支气管炎、哮喘和痛觉过敏等疾病研究中[3][4]。
体外实验中，MONNA（1μM；30秒）在分离的小鼠支气管平滑肌细胞中引起可重复的细胞内Ca2+浓度升高[5]。
体内实验中，MONNA（1μM；30分钟灌注）在Langendorff灌注的大鼠心脏中逆转了U46619诱导的冠脉流量减少[6]。MONNA（10μg/天；3天；SNL术后第4天开始；鞘内注射）减少了SNL诱导的大鼠损伤L5背根神经节中anoctamin-1、ATF-3和caspase-3蛋白表达的上调[7]。
| Cell experiment [1]: | |
Cell lines | Single airway smooth muscle cells |
Preparation Method | Single airway smooth muscle cells were isolated using a collagenase/proteinase mixture consisting of (per 5mL of Hanks Ca2+-free solution): 15mg/ml of collagenase (type II), 10mg/ml bovine serum albumin, 10mg/ml trypsin inhibitor and 1mg/ml proteinase. In order to examine the effects of MONNA on cytosolic [Ca2+] in isolated cells, MONNA (1μM) was applied three times for 30s. Cells were plated and incubated in 0.4μM fluo-4AM (Molecular Probes) for 6–8min at room temperature in Hank’s Ca2+-free solution to which 100μM Ca2+ was added. During experiments, dishes containing cells were continuously perfused with Hanks solution (Solution C) at 35±2℃. Additionally, the cell under study was continuously superfused with Hanks solution by means of a custom built close delivery system with a pipette tip diameter of 200μm placed approximately 300μm from the cell. The Hanks solution in the close delivery system could be switched to a drug-containing solution with a dead-space time of less than 5s. Cells were imaged using an iXon 887 EMCCD camera coupled to a Nipkow spinning disk confocal head. |
Reaction Conditions | 1μM; 30s |
Applications | MONNA caused reproducible elevations in intracellular Ca2+ concentration in isolated mouse bronchial smooth muscle cells. |
| Animal experiment [2]: | |
Animal models | Female Wistar rats |
Preparation Method | Female Wistar rats of 130-150g of weight (6-7 weeks) were housed in cages on a standard 12/12h light/dark cycle and had free access to food and water before experiments. Rats were sacrificed in a CO2 chamber at the end of experiments. Neuropathic pain was induced by L5/L6 spinal nerve ligation [SNL]. In order to determine the effect of MONNA in nerve injuryinduced neuropathic pain, rats were treated with MONNA (1-10μg; i.t.) or vehicle (1% or 15% DMSO; i.t.) daily for 3 days, starting on day 4 after nerve injury (SNL). Then, tactile allodynia was assessed from 7 to 21 days after injury. |
Dosage form | 1-10μg/day; 3 days; starting on day 4 after SNL; intrathecal injection |
Applications | MONNA reverted SNL-induced tactile allodynia in a dose-dependent manner in injured L5 dorsal root ganglia of rats. |
References: | |
| Cas No. | 1572936-83-4 | SDF | |
| 别名 | 2-(4-甲氧基萘-2-基氨基)-5-硝基苯甲酸 | ||
| 化学名 | 2-[(4-methoxy-2-naphthalenyl)amino]-5-nitro-benzoic acid | ||
| Canonical SMILES | COC1=CC(NC2=C(C(O)=O)C=C([N+]([O-])=O)C=C2)=CC3=CC=CC=C31 | ||
| 分子式 | C18H14N2O5 | 分子量 | 338.3 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: slightly soluble | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.956 mL | 14.7798 mL | 29.5596 mL |
| 5 mM | 591.2 μL | 2.956 mL | 5.9119 mL |
| 10 mM | 295.6 μL | 1.478 mL | 2.956 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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- Purity: >98.00%
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