Introduction：Basic information about CVN417 CAS 2919851-73-1, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
CVN417 Basic information
| Product Name: | CVN417 |
| Synonyms: | CVN417;1H-Pyrazole-3-carboxamide, 5-(2-chloro-4-methoxyphenyl)-1-methyl-N-[(3S)-1-methyl-3-piperidinyl]- |
| CAS: | 2919851-73-1 |
| MF: | |
| MW: | 362.85 |
| EINECS: | |
| Product Categories: | |
| Mol File: | 2919851-73-1.mol |
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CVN417 Chemical Properties
| Boiling point | 531.083±50.00 °C(Press: 760.00 Torr)(predicted) |
| density | 1.304±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) |
| pka | 8.519±0.20(predicted) |
Safety Information
CVN417 Usage And Synthesis
| Uses | CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease[1]. |
| in vivo | CVN417 (3 mg/kg, 10 mg/kg, 25 mg/kg; po) shows a dose-dependent decrease of tremulous jaw movement duration in Rat tacrine tremor model[1].
Pharmacokinetic Analysis of CVN417 in Rat Model[1]
| Route | Dose (mg/kg) | Cl (mL/min/kg) | Vdss (L/kg) | AUC0-∞ (ng·h/mL) | Cmax (μM) | F (%) | T1/2 (h) | Cbrain,total (2 h) | Kp, Kpu/u | | i.v. | 0.5 | 38.2 | 12.3 | 205 | | | | | | | p.o. | 10 | | | 0.35 | 775 | 11 | 5.9 | 1.82 | 4.1, 1.4 |
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| References | [1] Christie LA, et al. Discovery of CVN417, a Novel Brain-Penetrant α6-Containing Nicotinic Receptor Antagonist for the Modulation of Motor Dysfunction. J Med Chem. 2023 Aug 31. DOI:10.1021/acs.jmedchem.3c00630 |
CVN417 Preparation Products And Raw materials
