Yoda1

Yoda 1 是一种有效的选择性 Piezo1 激动剂。Yoda 1 激活纯化的 Piezo1 通道。Yoda 1 能有效抑制表皮生长因子 (EGF) 诱导的巨胞饮。Yoda 1 增强 Ca2+ 内流，随后激活钙激活钾通道 KCa3.1 和抑制 Rac1 激活。

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5mg

￥500.00

320.00

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10mg

￥1176.00

580.00

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25mg

￥2618.00

1000.00

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50mg

￥4188.00

0.00

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100mg

￥7137.00

0.00

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Yoda1 is a Piezo1 ion channel agonist (EC50s = 17.1 and 26.6 μM for murine and human Piezo1-transfected HEK293T cells, respectively).

货号：ajci20708
CAS：448947-81-7
分子式：C13H8Cl2N4S2
分子量：355.3
纯度：99%
存储：Store at -20°C
库存：现货

Background:

Yoda1 is a Piezo1 ion channel agonist (EC50s = 17.1 and 26.6 μM for murine and human Piezo1-transfected HEK293T cells, respectively).[1] It is selective for Piezo1 as it elicits Ca2+ flux in Piezo1- but not Piezo2-transfected HEK293T cells. Yoda1 slows the inactivation phase of murine Piezo1 transient currents and sensitizes them to activation by mechanical pressure, reducing the half maximal activation pressure by 15 mm Hg in an artificial droplet lipid bilayer. Treatment of wild-type red blood cells, but not Piezo1 knockout cells, with 15 μM yoda1 leads to dehydration and a change in cell shape resulting in progression from discocytes to echinocytes to spherocytes.[2]

参考文献：

1. Syeda, R., Xu, J., Dubin, A.E., et al. Chemical activation of the mechanotransduction channel Piezo1. Elife 4, e07369 (2015).

2. Cahalan, S.M., Lukacs, V., Ranade, S.S., et al. Piezo1 links mechanical forces to red blood cell volume. Elife 4, e07370 (2015).

Protocol

Cell experiment [1]:
Cell lines	Human coronary artery endothelial cells (HCAECs)
Preparation Method	Human coronary endothelial cells (HCAEC) were treated with the indicated concentration of Yoda1 for 5 min.
Reaction Conditions	1.5/3.0/6.0 µM for 5min
Applications	Yoda1 induced the activation of Akt and ERK1/2, and the increase of their respective phosphorylation levels reflected that the phosphorylation of the two signaling molecules also increased with the increase of Yoda1 concentration.
Animal experiment [2]:
Animal models	Eight-week-old SPF male C57BL/6 mice
Preparation Method	Hypertensive mice were injected with GSMTX-4, Yoda1 (Yod, 4 µg/kg/day) or LY294002 through tail vein for 3 days
Dosage form	4 µg/kg/day Yoda1 for 3 days
Applications	Agonist Yoda1 effectively inhibited calcium influx caused by hypertension. Antithrombotic studies proved that the inhibition of Piezo1 effectively inhibited arterial thrombosis and reduced the infarct size of stroke in hypertensive mice.
References: [1]: Dela Paz NG, Frangos JA. Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation. Biochem Biophys Res Commun. 2018 Feb 26;497(1):220-225. doi: 10.1016/j.bbrc.2018.02.058. Epub 2018 Feb 8. PMID: 29428723; PMCID: PMC5835220. [2]: Zhao W, Wei Z, et,al. Piezo1 initiates platelet hyperreactivity and accelerates thrombosis in hypertension. J Thromb Haemost. 2021 Dec;19(12):3113-3125. doi: 10.1111/jth.15504. Epub 2021 Oct 8. PMID: 34411418.