Molecular Formula | C18H28ClN3O3 |
Molar Mass | 369.9 |
Solubility | DMSO: ≥10mg/mL |
Appearance | powder |
Color | white to off-white |
Storage Condition | Inert atmosphere,2-8°C |
In vitro study | VU0357017 is selective for M 1 (K i =9.91 µM) over M 2 -M 5 mAChRs (K i =21.4, 55.3, 35.0, and 50.0 μM, respectively) in CHO cells. VU0357017 (1 nM-100 μM) induces calcium release and ERK phosphorylation in a concentration-dependent manner in CHO cells. |
Hazard Symbols | N - Dangerous for the environment |
Risk Codes | 52/53 - Harmful to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | 61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
WGK Germany | 2 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.704 ml | 13.518 ml | 27.035 ml |
5 mM | 0.541 ml | 2.704 ml | 5.407 ml |
10 mM | 0.27 ml | 1.352 ml | 2.704 ml |
5 mM | 0.054 ml | 0.27 ml | 0.541 ml |
biological activity | VU0357017 hydrochloride (CID-25010775) is a potent, central nervous system permeability highly selective M1 agonists, M1 is a class of subtypes of muscarinic acetyl linear receptors (mAChRs). VU0357017 hydrochloride acts at the allosteric site to activate the receptor with an EC50 value of 477 nM and a Ki value of 9.91 μm. |
Target | Value |
M1 mAChR (Cell-free assay) | 477 nM(EC50) 9.91 μM(Ki) |
Animal Model: | Male Sprague−Dawley rats (380-420 g) were pretreated with scopolamine |
Dosage: | 1, 3, 10 mg/kg |
Administration: | A single i.p. |
Result: | Produced a significant reversal of the scopolamine-induced deficits at a dose of 10 mg/kg. |