Yoda 1

Selective mouse and human Piezo1 channel activator which does not show modulatory effects on Piezo2 (EC₅₀ values = ~10-50 µM). Activates Piezo1 without application of any mechanical force and binds to a narrow hydrophobic pocket to stabilize the open conformation of the channel. Shows various activities including elevation of intracellular calcium levels, control volume of red blood cells, activation of PI3K-Akt signaling, enhancement of human aortic smooth muscle cell lines calcification and increase bone mass in vivo.

Yoda2 (KC289) and KC159 are more efficacious, potent and Piezo1 activators with improved solubility in aqueous solutions.

2-[5-[[(2,6-Dichlorophenyl)methyl]thio]-1,3,4-thiadiazol-2-yl]pyrazine