Date published: 2025-9-14

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TMEM16H Activators

TMEM16H activators predominantly function by influencing intracellular calcium levels or pathways that result in the modification of these levels. These compounds, upon influencing these pathways, can enhance the functional activity of TMEM16H. For instance, Forskolin, an activator of adenylyl cyclase, and IBMX can increase intracellular cAMP levels. The elevated cAMP levels can activate protein kinase A, which in turn can phosphorylate and activate TMEM16H. Similarly, UTP and ATP can activate P2Y receptors, leading to the production of IP3 and DAG through the phospholipase C pathway, indirectly enhancing the activity of TMEM16H.

Moreover, other compounds like Ouabain, Thapsigargin, A23187, Genistein, Glyburide, Verapamil, BAPTA-AM, and Nifedipine can also influence intracellular calcium levels, leading to the enhanced functional activity of TMEM16H. For example, Ouabain inhibits the sodium-potassium ATPase pump, which can lead to an increase in intracellular calcium levels, enhancing the activity of TMEM16H. Thapsigargin causes an increase in cytosolic calcium levels, enhancing the activity of TMEM16H.

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