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General description
An N-aroylaminothiazole that strongly activates TMEM16A (ANO1) calcium-activated chloride channel (CaCC) at 0 Ca2+ concentration (Ca2+ independent), with the capability of producing large and sustained CaCC Cl-1 currents (EC50 = 3 µM) in TMEM16A-expressing Fisher Rat Thyroid (FRT) Cells without elevation of cytoplasmic Ca2+ level, and in human A253 cells. Shown to increase CaCC conductance in human salivary and airway submucosal gland epithelial cells, IL-4 treated bronchial cells, and stimulated submucosal gland secretion in human bronchi and smooth muscle contraction in mouse intestine. Activation effect can be abolished by the addition of a TMEM16A inhibitor T16A-A01 at 10 µM in TMEM16A-transfected cells and in cultures of human salivary gland and IL-4-treated bronchial epithelia, but not in intestine. Does not affect CFTR Cl- conductance or ENaC Na+ conductance.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Namkung, W., et al. 2011. FASEB J.25, 4048.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white |
| solubility | DMSO: 100 mg/mL, clear, colorless |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | [s]1c(nc(c1)c3ccccc3)N(CCOC)C(=O)c2cc(c(c(c2)OC)OC)OC |
| InChI | 1S/C22H24N2O5S/c1-26-11-10-24(22-23-17(14-30-22)15-8-6-5-7-9-15)21(25)16-12-18(27-2)20(29-4)19(13-16)28-3/h5-9,12-14H,10-11H2,1-4H3 |
| InChI key | ZUXNHFFVQWADJL-UHFFFAOYSA-N |
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