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Yoda 1

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Chemical Structure| 448947-81-7 同义名 : -
CAS号 : 448947-81-7
货号 : A458265
分子式 : C13H8Cl2N4S2
纯度 : 99%+
分子量 : 355.265
MDL号 : MFCD00833175
存储条件:

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 15 mg/mL(42.22 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 5 mg/mL(14.07 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方:
生物活性
描述 Piezo1 protein, encoded by PIEZO1 gene, is a mechanically-activated ion channel that links mechanical forces to biological signals. Piezo1 contains 36 transmembrane domains and functions as a homotetramer. Piezo1 plays a key role in epithelial cell adhesion by maintaining integrin activation through R-Ras recruitment to the ER, most probably in its activated state, and subsequent stimulation of calpain signaling. Moreover, Piezo1 acts as shear-stress sensor that promotes endothelial cell organization and alignment in the direction of blood flow through calpain activation and it plays a key role in blood vessel formation and vascular structure in both development and adult physiology. GlyT2-IN-1, also termed ‘Yoda-1’, is an agonist for both human and mouse Piezo1, with EC50 values of 26.6 μM and 17.1μM for human and mouse Piezo1, respectively[3]. In HEK293T cells transiently transfected with mouse Piezo1, Yoda-1 mediated Ca2+ responses at the concentration of 25 μM, and this effect depended on calcium influx as the chelation of extracellular calcium dramatically reduced the responses and the depletion of intracellular calcium stores did not. Also in mouse Piezo1 transfected HEK293T cells, using a cell attached patch configuration, it was measured that Yoda-1 notably slowed the inactivation phase of the transient currents at the concentration of 30 μM. Utilizing artificial droplet lipid bilayers, it was shown that Yoda-1 activated purified Piezo1 channels in the absence of other cellular components at the concentration of 1 μM[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.07mL

2.81mL

1.41mL

28.15mL

5.63mL

2.81mL

参考文献

[1]Syeda R, Xu J, Dubin AE, et al. Chemical activation of the mechanotransduction channel Piezo1. Elife. 2015

[2]Mikhailov N, Leskinen J, Fagerlund I, et al. Mechanosensitive meningeal nociception via Piezo channels: Implications for pulsatile pain in migraine?. Neuropharmacology. 2019

[3]Syeda R, Xu J, Dubin AE, Coste B, Mathur J, Huynh T, Matzen J, Lao J, Tully DC, Engels IH, Petrassi HM, Schumacher AM, Montal M, Bandell M, Patapoutian A. Chemical activation of the mechanotransduction channel Piezo1. Elife. 2015 May 22;4:e07369.