VU0357017 hydrochloride is a highly selective M1 agonist. VU0357017 hydrochloride acts at an allosteric site to activate the receptor. Ki values of VU0357017 derived from competition binding experiment is 9.91(rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), respectively. VU0357017 has robust effects on M1-activation of calcium mobilization and ERK1/2 phosphorylation but have little effect on β-arrestin recruitment. VU0357017 HCl induces calcium release and ERK phosphorylation but is without effects on β-arrestin recruitment. VU0357017 HCl enhances performance in Morris water maze and contextual fear conditioning in rats.
| Molecular Weight | 369.89 |
| Formula | C18H28ClN3O3 |
| CAS Number | 1135242-13-5 |
| Solubility (25°C) | DMSO 24 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.
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