T16Ainh - A01
目录号 : GC17930
An inhibitor of TMEM16A channels
Cas No.:552309-42-9
Sample solution is provided at 25 µL, 10mM.
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Transmembrane protein 16A (TMEM16A, also known as anoctamin-1) is a calcium-activated chloride channel (CaCC) with roles in transepithelial anion transport and smooth muscle contraction. T16A(inh)-A01 is an aminophenylthiazole that inhibits transient TMEM16A-mediated chloride currents with an IC50 value of ~1 µM.[1],[2] Its inhibitory effects are independent of voltage and do not prolong the rate of TMEM16A current deactivation.[2]T16A(inh)-A01 blocks CaCC activity in vascular smooth muscle cells and relaxes mouse and human blood vessels.[3] It also inhibits the proliferation of pancreatic cancer and squamous carcinoma cells in culture.[4],[5]
Reference:
[1]. Namkung, W., Phuan, P.W., and Verkman, A.S. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells. The Journal of Biological Chemisty 286(3), 2365-2374 (2011).
[2]. Bradley, E., Fedigan, S., Webb, T., et al. Pharmacological characterization of TMEM16A currents. Channels 8(4), 308-320 (2014).
[3]. Davis, A.J., Shi, J., Pritchard, H.A.T., et al. Potent vasorelaxant activity of the TMEM16A inhibitor T16Ainh-A01. British Journal of Pharmacology 168, 773-784 (2013).
[4]. Mazzone, A., Eisenman, S.T., Strege, P.R., et al. Inhibition of cell proliferation by a selective inhibitor of the Ca2+ activated Cl- channel, Ano1. Biochemical and Biophysical Research Communications 427(2), 248-253 (2012).
[5]. Duvvuri, U., Shiwarski, D.J., Xiao, D., et al. TMEM16A induces MAPK and contributes directly to tumorigenesis and cancer progression. Cancer Research 72(13), 3270-3281 (2012).
| Cell experiment [1]: | |
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Cell lines |
Rabbit pulmonary artery myocytes |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
Whole cell IClCa were evoked by pipette solution which had the following composition (in mM): TEA (20), CsCl (106), HEPES-CsOH (10, pH 7.2), BAPTA (10), ATP.Mg (5) and GTP.diNa (0.2). To this solution, 7.08 mM CaCl2 were added to achieve a free [Ca2+] of 500 nM. The bathing solution had the following composition (in mM): NaCl (126), HEPES-NaOH (10, pH 7.35), TEA (8.4), glucose (20), MgCl2 (1.2) and CaCl2 (1.8). The effect of T16Ainh-A01 (1–30 μM) was studied on IClCa evoked by 500 nM free Ca2+. |
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Applications |
In rabbit pulmonary artery myocytes T16Ainh-A01 (1–30 μM) inhibited single calcium (Ca2+)-activated whole cell currents activated by 500 nM free Ca2+. |
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References: [1] Alison J Davis, et al. Potent vasorelaxant activity of the TMEM16A inhibitor T16Ainh-A01. Br J Pharmacol. 2013 Feb; 168(3): 773–784. |
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| Cas No. | 552309-42-9 | SDF | |
| 化学名 | 2-((5-ethyl-6-methyl-4-oxo-1,4-dihydropyrimidin-2-yl)thio)-N-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide | ||
| Canonical SMILES | O=C1N=C(NC(C)=C1CC)SCC(NC2=NC(C(C=C3)=CC=C3OC)=CS2)=O | ||
| 分子式 | C19H20N4O3S2 | 分子量 | 416.52 |
| 溶解度 | 5mg/ml in DMSO; 10mg/ml in DMF | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4008 mL | 12.0042 mL | 24.0085 mL |
| 5 mM | 0.4802 mL | 2.4008 mL | 4.8017 mL |
| 10 mM | 0.2401 mL | 1.2004 mL | 2.4008 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。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet