piezochannel

D-GsMTx4 TFA belongs to natural products and is a TRPC1/6 and Piezo2 channel inhibitor with high selectivity and cell permeability, inhibiting Ca2+ influx and the mTOR pathway. This compound is used in research on myocardial infarction, chronic pain, and pulmonary fibrosis.

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1/26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

GsMTx4 TFA (1209500-46-8 free base) is a spider venom peptide that selectively inhibits cation permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families.

Dooku1 is an analog of Yoda1 and a selective antagonist of endogenous Piezo1 channels. Dooku1 inhibits Ca2+ entry induced by 2μMYoda1 with IC50 values of 1.3μM (in HEK 293 cells) and 1.5μM (in HUVEC). Dooku1 inhibits Yoda1-induced aortic relaxation.

Jedi2 is a Piezo1 activator rather than a specific Piezo2 activator. Jedi2 binds to the mouse Piezo1 proteins with a K d of 2770 μM [1].

MCB-22-174 is a potent agonist of Piezo1 with an EC50 value of 6.28 µM. It activates Ca2+-related extracellular signal-regulated kinase and calcium-calmodulin (CaM)-dependent protein kinase II (CaMKII) pathways, and it promotes mesenchymal stem cell osteogenic differentiation, indicating its potential application in the study of disuse osteoporosis (OP).

Yoda2 (KC289), the potassium salt of Yoda1, is an agonist of PIEZO1 with an EC50 of 150 nM. It induces Ca2+ elevation in HeLa cells and can cause concentration-dependent and NO-dependent relaxation in mouse portal vein (EC50= 1.2 μM). Additionally, Yoda2 is capable of stimulating NOS3 and promoting NO production.

TRPC1/6 and Piezo2 inhibitor. Exhibits same effect as L-enantiomer, GsMTx4 (Cat. No. 4912) on TRPC channels. Inhibits mechanosensitive currents by ~70%. Protects against myocardial infarction in mouse ischemia/reperfusion model. Resistant to proteolytic digestion.