2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. CVN417

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.

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CVN417 Chemical Structure

CVN417 Chemical Structure

CAS No. : 2919851-73-1

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CVN417 Related Antibodies

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Description

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].

IC50 & Target

IC50: 0.086 μM (nAChR α6), 2.56 μM (nAChR α3), 0.657 μM (nAChR α4)[1]
In Vitro

CVN417 (10 μM; 0-2 h) shows low metabolic turnover in human liver microparticles or hepatocytes[1].

In Vitro ADME Data for CVN417[1]

human rat mouse dog
liver microsomes Clint (μL/min/mg) 2.8 31.2 33.3 27.7
hepatocytes (mL/min/106 cells) 3.7 20.8 25.1 32.3

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CVN417 Related Antibodies
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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

362.85

Formula

C18H23ClN4O2
CAS No.
SMILES

ClC1=C(C=CC(OC)=C1)C2=CC(C(N[C@@H]3CN(CCC3)C)=O)=NN2C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CVN417 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CVN4172919851-73-1CVN 417CVN-417nAChRNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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