Piezo Channel

GsMTX4 is a 34 amino acid peptidyl toxin isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family.

Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel.

Yoda 1 is a Piezo1 agonist. Yoda 1 activates purified Piezo1 channels.

Piezo1 agonist 1-d2 is a selective agonist for the Piezo1 ion channel, exhibiting an EC50 of 2.21 μM. This compound activates Ca2+-dependent ERK signaling pathways, thereby facilitating the osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs). Additionally, Piezo1 agonist 1-d2 has demonstrated efficacy in ameliorating disuse osteoporosis in hindlimb-unloading rat models, making it a valuable tool for research in bone health and regenerative medicine.

MCB-22-174 is a deuterated agonist of the Piezo1 mechanosensitive ion channel, exhibiting an EC50 of 6.28 μM. This compound effectively activates the CaMKII/ERK signaling pathway and promotes calcium influx in rat mesenchymal stem cells (rMSCs). MCB-22-174 reduces the expression of chondrogenic markers, such as Comp and Acan, alongside adipogenic markers including Lpl and Fabp4. This reagent has potential applications in enhancing bone quality in models of disuse osteoporosis, making it a valuable tool for research in skeletal health and regenerative medicine.

Jedi2 is a selective activator of the Piezo1 ion channel, facilitating mechanotransduction in various physiological processes. It demonstrates a binding affinity (Kd) of 2770 μM for mouse Piezo1 proteins, enabling the study of Piezo1's role in cellular responses to mechanical stimuli. This compound is suitable for research applications investigating the physiological and pathological implications of Piezo1 activation in multiple biological systems.

Yaddle1 is a potent agonist of the mechano-activated ion channel Piezo1, exhibiting a half-maximal effective concentration (MEC50) of 0.40 μM. This compound effectively promotes Ca2+ influx in T cells, leading to significant T cell activation. Yaddle1 serves as a valuable tool in research applications focused on vaccine adjuvants and the modulation of immune responses.

Yoda2 (KC289) functions as a Piezo1 agonist with an EC50 of 150 nM, facilitating calcium ion elevation and nitric oxide-dependent relaxation. This compound induces vasodilation in mouse arterial and cavernous tissues. Additionally, Yoda2 is implicated in inhibiting glucocorticoid-induced osteoclast formation and bone resorptive activity, effectively reversing glucocorticoid-mediated bone density loss and structural deterioration. Its applications extend to research in areas such as hypertension and osteoporosis.