TMEM16A Activator, Eact

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.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Namkung, W., et al. 2011. FASEB J.25, 4048.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)