Uses
This 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.
Uses
T16Ainh-A01 has been used as an inhibitor of transmembrane protein 16A (TMEM16A).
Uses
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.
General Description
An aminophenylthiazole that acts as an inhibitor of TMEM16A channel, a calcium-activated chloride channel (CaCC) (IC
50 = 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.
Biochem/physiol Actions
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.
