1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. Piezo Channel

Piezo Channel

Piezo channels are the trimeric mechanosensitive ion channels that open in response to mechanical stimuli such as shear stress and membrane stretch, allowing positively charged ions, including calcium, to flow into the cell. It is speculated that extracellular mechanical stimuli can be converted into tension from lipid molecules in the cell membrane to activate the Piezo channels. The intracellular beam might transmit tension from lipid molecules from the distal blade to the central pore module by means of a lever principle, which opens the central pore for ion-conducting. Most vertebrates have two channel isoforms, Piezo1 and Piezo2. Piezo1 and Piezo2 are involved in various mechanotransduction pathways, including touch sensation, proprioception, nociception, vascular development, and breathing. In humans, gain-of-function mutations in Piezo1 are linked to dehydrated hereditary stomatocytosis (DHS). Loss-of-function mutations in Piezo1 and Piezo2 are linked to congenital lymphatic dysplasia14 and defective touch perception and proprioception.

Piezo Channel Related Products (13):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18723
    Yoda 1
    Agonist 99.97%
    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.
    Yoda 1
  • HY-P1410
    GsMTx4
    Inhibitor 99.89%
    GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
    GsMTx4
  • HY-126010
    Dooku1
    Antagonist 99.93%
    Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research.
    Dooku1
  • HY-P1410A
    GsMTx4 TFA
    Inhibitor 99.85%
    GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
    GsMTx4 TFA
  • HY-P1410B
    D-GsMTx4
    Inhibitor 99.44%
    D-GsMTx4 is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 inhibits [Ca2+]i elevation. D-GsMTx4 inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.
    D-GsMTx4
  • HY-181743
    Piezo1 agonist 2
    Agonist
    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.
    Piezo1 agonist 2
  • HY-181467
    KC159
    Agonist
    KC159 is a Yoda1 analog, as well as an agonist of Piezo1 and Piezo2. KC159 can be used for cultured adipocyte production.
    KC159
  • HY-P1410C
    D-GsMTx4 TFA
    Inhibitor 99.89%
    D-GsMTx4 TFA is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 TFA inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 TFA inhibits [Ca2+]i elevation. D-GsMTx4 TFA inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 TFA inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 TFA can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.
    D-GsMTx4 TFA
  • HY-131018
    Jedi2
    99.93%
    Jedi2 is a Piezo1 activator, but not a specific Piezo2 activator. Jedi2 binds to the mouse Piezo1 proteins with a Kd of 2770??μM.
    Jedi2
  • HY-162501
    Yaddle1
    Agonist 99.98%
    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.
    Yaddle1
  • HY-175416
    Yoda2
    Agonist 99.57%
    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.
    Yoda2
  • HY-165607S
    MCB-22-174
    Agonist 99.78%
    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).
    MCB-22-174
  • HY-169332
    Piezo1 agonist 1-d2
    Agonist
    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.
    Piezo1 agonist 1-d<sub>2</sub>