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.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PL09845 | Dooku1 | 2253744-54-4 | Dooku1 是Yoda1 的一个类似物,是选择性的、内源性的 Piezo1通道的拮抗剂,在HEK 293 细胞以及HUVEC 中测得对2 μM Yoda1 诱导的钙离子流的IC50 值分别为1.3 μM 和1.5 μM。Dooku1 抑制Yoda1 诱导的主动脉舒张。 |
PL09489 | GsMTx4 TFA | GsMTx4 TFA 是一种蜘蛛毒液肽,选择性地抑制属于 Piezo 和 TRP 通道家族的阳离子可渗透的机械敏感性通道 (MSCs)。GsMTx4 TFA 还可阻断阳离子选择性的拉伸激活通道 (SAC),减弱溶血磷脂酰胆碱 (LPC) 诱导的星形胶质细胞毒性和小胶质细胞反应性。GsMTx4 TFA 是一种重要的药理学工具,可用于鉴定兴奋性 MSCs 在正常生理学和病理学中的作用。 | |
PC22098 | GsMTx4 TFA盐 | 1209500-46-8 | |
PC22099 | GsMTx4 醋酸盐 | 1209500-46-8 | |
PL09844 | Jedi2 | 651005-90-2 | Jedi2 是一种 Piezo1 活化剂,但不是 Piezo2 活化剂。Jedi2 与小鼠 Piezo1 蛋白结合,Kd 值为 2770 μM。 |