552309-42-9

TMEM16AInhibitorsRevealTMEM16A(T16Ainh-A01)  compound functions as a selective class A inhibitor of the calcium activated chloride channel TMEM16A. Useful in the treatment of hypertension, pain, diarrhea and mucus overproduction.

An aminophenylthiazole that acts as an inhibitor of TMEM16A channel, a calcium-activated chloride channel (CaCC) (IC₅₀ = 1.1 μM). Fully blocks CaCC current in salivary gland cells at 10 μM, but has very little effect in airway and intestinal cells, which is consistent with the observation of RNAi knock-down. Completely blocks chloride currents produced by TMEM16A Activator, Eact (Cat. No. 631547) at 10 μM. In addition, shown to block calcium-activated chloride channels in vascular smooth muscle cells, and relaxes murine and human blood vessels.

T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells. T16Ainh-A01 poorly inhibited total CaCC current in intestinal and airway epithelial cells, but blocked mainly an initial, agonist-stimulated transient chloride current. T16Ainh-A01 does not alter cytoplasmic calcium and has little effect on CFTR Cl- conductance.

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