Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation. Yoda1 acts by eliciting Ca2+ flux in Piezo1- but not vector-transfected cells. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF).
Glia. 2023 Jan 4.
Mechanosensitive channel Piezo1 is an essential regulator in cell cycle progression of optic nerve head astrocytes
Yoda1 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | - |
| Preparation method | Calcium imaging Pancreatic acini were plated on glass coverslips pre-treated with Cell-Tak (Corning). Cells were loaded Calcium 6-QF (Molecular Devices) in minimum essential medium:Hanks’ balanced salt solution (MEM:HBSS; 1:1) for 1 h at 37 °C in a CO2 incubator. Prior to imaging, MEM:HBSS media were replaced by HBSS with 2 mM Ca2+. Imaging was performed at room temperature using a Zeiss Axio observer Z1 with a ×20 objective. Images were recorded every 400 ms over 3 min and data were analyzed using MetaMorph software (Molecular Devices). Yoda1 resuspended in DMSO at 50 mM was added at a final concentration of 25 µM in HBSS media. Yoda1 was added 30 s from the start of the recording. When GsMTx4 was tested on acini, the cells were preincubated with GsMTx4 (2.5 µM) 2 min prior to recording. Overloaded or faintly fluorescent acini (F0 < 150 AI) were excluded from the analysis as well as cells demonstrating unstable fluorescence before loading. |
| Concentrations | 25 µM |
| Incubation time | - |
| Animal Experiment | |
|---|---|
| Animal models | 5-month-old transgenic 5xFAD male mice with fully developed Aβ pathology |
| Formulation | 1% DMSO in saline |
| Dosages | 5 µl (0.25 µg/mouse/day), 10 infusions over a period of 12 days |
| Administration | cannula infusions |
| Molecular Weight | 355.27 |
| Formula | C13H8Cl2N4S2 |
| CAS Number | 448947-81-7 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Syeda R, et al. Elife. Chemical activation of the mechanotransduction channel Piezo1.
| Related Piezo Channel Products |
|---|
| Jedi2
Jedi2 is a Piezo1 activator, but not a specific Piezo2 activator. Jedi2 binds to the mouse Piezo1 proteins with a Kd of 2770 μM. |
| Dooku1
Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibits 2 μM Yoda1-induced Ca2+Incoming, IC50 values in HEK 293 cells and HUVECs are 1.3 μM and 1.5 μM, respectively. |
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