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.
| Molecular Weight | 326.2 |
| Formula | C13H9Cl2N3OS |
| CAS Number | 2253744-54-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage | -20°C, dry, sealed |
| 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.
| 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. |
| Yoda1
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). |
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