Piezo Channel (Inhibitors Agonists Modulators Antagonists)

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Membrane transporter/Ion channel

Monoamine Transporter

(54)

Monocarboxylate transporter

Na-K-Cl cotransporter

Sodium-dependent phosphate transporter

Piezo Channel

PIEZO1 is a mechanosensitive ion channel protein that in humans is encoded by the gene PIEZO1. PIEZO1 is expressed in the lungs, bladder and skin, where mechanosensation has important biological roles. Unlike PIEZO2 which is highly expressed in sensory dorsal root ganglia, PIEZO1 is not expressed in sensory neurons. Consequently, PIEZO1 plays a significant role in multiple neurobiological processes including axon regeneration, neural stem cells differentiation and neurological disease progression.

GsMTx4 TFA (1209500-46-8 free base)

GsMTx4 TFA

TP1300

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.

Piezo Channel

$312

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D-GsMTx4 TFA

T37697L

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.

Akt Calcium Channel mTOR PI3K Piezo Channel TRP/TRPV Channel

$163

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Yoda 1

T7506448947-81-7

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).

Akt ERK Piezo Channel Potassium Channel

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Dooku1

T110762253744-54-4

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.

Piezo Channel

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Jedi2

Fr13138651005-90-2

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].

Others Piezo Channel

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MCB-22-174

T2077933058199-58-6

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).

CaMK ERK Others Piezo Channel

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10-14 weeks

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Yaddle1

T210349

Yaddle1 is an agonist of the mechanically sensitive ion channel protein Piezo1, with a half-maximal effective concentration (MEC50) of 0.40 μM. It significantly induces Ca2+ influx in T cells, prompting T cell activation responses. Yaddle1 is applicable in vaccine adjuvant research.

Piezo Channel

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Yoda2

KC289

T2116833081450-95-2

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.

NO Synthase Piezo Channel

$1,520

6-8 weeks

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D-GsMTx4

T37697

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.

Piezo Channel

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