T16Ainh - A01 |
| Catalog No.GC17930 |
Inhibit transient TMEM16A-mediated chloride currents
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | 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 | ||
| Formula | C19H20N4O3S2 | M.Wt | 416.52 |
| Solubility | 5mg/ml in DMSO; 10mg/ml in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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