| 货号 | 18518-5mg |
| 描述 | 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 |
| 供应商 | Cayman |
| 应用文献 | |
| 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). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 416.5 |
| 分子式 | C19H20N4O3S2 |
| CAS号 | 552309-42-9 |
| 稳定性 | ≥ 2 years |
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