Piezo Channel Agonist

Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca²⁺ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.

KC159 is a Yoda1 analog, as well as an agonist of Piezo1 and Piezo2. KC159 can be used for cultured adipocyte production.

Piezo1 agonist 2 (Compound PD2) is a blood-brain barrier-permeable Piezo1 agonist and Jedi2 (HY-131018) conjugate that utilizes LAT1. Piezo1 agonist 2 releases Jedi2 in mice. Piezo1 agonist 2 can be used for the research of neurodegenerative diseases.

Yaddle1 is an agonist of the mechano-activated ion channel (Piezo1) with a half-maximal effective concentration (MEC₅₀) of 0.40 μM. Yaddle1 can significantly trigger Ca²⁺ inflow in T cells and induce T cell activation response. Yaddle1 can be used in the study of vaccine adjuvants.

Yoda2 (KC289), the potassium salt of Yoda1 (HY-18723), is a PIEZO1 agonist with an EC₅₀ of 150 nM. Yoda2 evokes Ca²⁺ elevation and NO-dependent relaxation. Yoda2 induces relaxation in mouse arterial and cavernous tissues. Yoda2 inhibits glucocorticoid-induced osteoclast formation and bone resorptive activity, reverses glucocorticoid-induced bone density loss and architectural deterioration, and does not induce medication-related osteonecrosis of the jaw in mice. Yoda2 can be used for the researches of hypertension and osteoporosis.

MCB-22-174 is a deuterated Piezo1 agonist, with an EC₅₀ value of 6.28 μM. MCB-22-174 remarkably activates the CaMKII/ERK signaling pathway and initiates Ca²⁺ influx in rMSCs. MCB-22-174 significantly decreases the expression of chondrogenesis markers (Comp, Acan) and adipogenesis markers (Lpl, Fabp4) in MSCs. MCB-22-174 can effectively improve bone quality in hind-limb unloading (HU) model rats. MCB-22-174 can be used for the study of disuse osteoporosis (OP).

Piezo1 agonist 1-d2 is a Piezo1 agonist and osteogenesis promoter with an EC₅₀ of 2.21 μM. Piezo1 agonist 1-d2 activates Piezo1 and induces calcium ion influx in mesenchymal stem cells. Piezo1 agonist 1-d2 activates the Erk signaling pathway and promotes osteogenesis of mesenchymal stem cells. Piezo1 agonist 1-d2 alleviates disuse osteoporosis in a hindlimb unloading rat model. Piezo1 agonist 1-d2 can be used for research on osteoporosis.