Ani 9是一种高选择性的ANO1抑制剂,可有效阻断ANO1通道活性,对ANO1的IC₅₀值小于3μM。
Cas No.:356102-14-2
Sample solution is provided at 25 µL, 10mM.
Ani 9 is a highly selective inhibitor of ANO1 that potently blocks ANO1 channel activity with an IC₅₀ below 3μM. Ani 9 did not affect the intracellular calcium signaling and CFTR chloride channel activity. Ani 9 may be a useful pharmacological tool for studying ANO1 and a potential development candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma[1].
In vitro, treatment with 3-30μM Ani 9 for 24-72h inhibited PC-3 cell growth in dose-dependent and time-dependent manner[2]. Application of Ani 9 up to 30μM for 20min did not affect the ATP-induced cytosolic calcium increase in FRT cells[1]. 1μM, 3μM and 10μM Ani 9 for 20min inhibited VRAC activity by 13.5±1.1%, 21.4±1.0% and 40.7±1.5%, respectively in LN215[1]. 3μM Ani9 for 30min did not affect electrical field stimulation (EFS)-evoked contractions of male murine USM[3]. 10μM Ani 9 for 30min had no blocking effect on contractures of mouse bronchi induced by carbachol[4].
References:
[1] Seo Y, Lee HK, Park J, et al. Ani9, A Novel Potent Small-Molecule ANO1 Inhibitor with Negligible Effect on ANO2. PLoS One. 2016;11(5):e0155771.
[2] Song Y, Gao J, Guan L, Chen X, Gao J, Wang K. Inhibition of ANO1/TMEM16A induces apoptosis in human prostate carcinoma cells by activating TNF-α signaling. Cell Death Dis. 2018;9(6):703.
[3] Gupta N, Baker SA, Sanders KM, et al. ANO1 channels are expressed in mouse urethral smooth muscle but do not contribute to agonist or neurally evoked contractions. Sci Rep. 2025;15(1):17365.
[4] 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.
Ani 9是一种高选择性的ANO1抑制剂,可有效阻断ANO1通道活性,对ANO1的IC₅₀值小于3μM。Ani 9不影响细胞内钙信号传导和CFTR氯离子通道活性。Ani 9可能是一种有用的药理学工具,用于研究ANO1,并有望成为治疗癌症、高血压、疼痛、腹泻和哮喘的潜在药物候选物[1]。
体外实验中,3-30μM的Ani 9处理PC-3细胞24-72小时,PC-3细胞的活性以剂量依赖和时间依赖的方式被抑制[2]。30μM的Ani 9处理FRT细胞20分钟,不影响ATP诱导的细胞质钙升高[1]。在LN215细胞中,1μM、3μM和10μM的Ani 9处理20分钟,对VRAC的活性抑制率分别在13.5±1.1%、21.4±1.0%和40.7±1.5%[1]。3μM的Ani 9处理30分钟,不影响电场刺激(EFS)诱导的雄性小鼠尿道平滑肌的收缩[3]。10μM的Ani 9处理30分钟,对卡巴胆碱诱导的小鼠支气管收缩没有阻断作用[4]。
| Cell experiment [1]: | |
Cell lines | PC-3 cell |
Preparation Method | PC-3 cells were treated with different concentrations of Ani9 for 24-72h. Cell proliferation was measured by CCK-8 assay. |
Reaction Conditions | 3-30μM; 24-72h |
Applications | Ani 9 inhibited cell growth in dose-dependent and time-dependent manner. |
References: | |
| Cas No. | 356102-14-2 | SDF | |
| 化学名 | 2-(4-chloro-2-methylphenoxy)-acetic acid, 2-[(2-methoxyphenyl)methylene]hydrazide | ||
| Canonical SMILES | ClC1=CC=C(OCC(N/N=C/C2=CC=CC=C2OC)=O)C(C)=C1 | ||
| 分子式 | C17H17ClN2O3 | 分子量 | 332.8 |
| 溶解度 | 25mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0048 mL | 15.024 mL | 30.0481 mL |
| 5 mM | 601 μL | 3.0048 mL | 6.0096 mL |
| 10 mM | 300.5 μL | 1.5024 mL | 3.0048 mL |
| 第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
| 给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
| 第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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