CVN417
Based on 1 Customer Validation
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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- Purity: 99.93%
- CAS No.: 2919851-73-1
- 화학식: C18H23ClN4O2
- 분자량:362.85
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Orally Active Compound Library
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Neurotransmitter Receptor Compound Library
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Anti-Parkinson's Disease Compound Library
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Neurodegenerative Disease-related Compound Library
HY-L086
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Antidepressant Compound Library
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Membrane Protein-targeted Compound Library
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Membrane Receptor-targeted Compound Library
HY-L150
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Ion Channel Compound Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Bioactive Compound Library
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
IC50: 0.086 μM (nAChR α6), 2.56 μM (nAChR α3), 0.657 μM (nAChR α4)[1]
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.
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.
Chemical Information
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CAS No. 2919851-73-1
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Appearance Solid
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분자량 362.85
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화학식 C18H23ClN4O2
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Color White to off-white
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SMILES
ClC1=C(C=CC(OC)=C1)C2=CC(C(N[C@@H]3CN(CCC3)C)=O)=NN2C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (275.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7560 mL | 13.7798 mL | 27.5596 mL | 68.8990 mL |
| 5 mM | 0.5512 mL | 2.7560 mL | 5.5119 mL | 13.7798 mL | |
| 10 mM | 0.2756 mL | 1.3780 mL | 2.7560 mL | 6.8899 mL | |
| 15 mM | 0.1837 mL | 0.9187 mL | 1.8373 mL | 4.5933 mL | |
| 20 mM | 0.1378 mL | 0.6890 mL | 1.3780 mL | 3.4449 mL | |
| 25 mM | 0.1102 mL | 0.5512 mL | 1.1024 mL | 2.7560 mL | |
| 30 mM | 0.0919 mL | 0.4593 mL | 0.9187 mL | 2.2966 mL | |
| 40 mM | 0.0689 mL | 0.3445 mL | 0.6890 mL | 1.7225 mL | |
| 50 mM | 0.0551 mL | 0.2756 mL | 0.5512 mL | 1.3780 mL | |
| 60 mM | 0.0459 mL | 0.2297 mL | 0.4593 mL | 1.1483 mL | |
| 80 mM | 0.0344 mL | 0.1722 mL | 0.3445 mL | 0.8612 mL | |
| 100 mM | 0.0276 mL | 0.1378 mL | 0.2756 mL | 0.6890 mL |
CVN417 Related Classifications
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