Solangepras
Based on 1 publication(s) in Google Scholar
CVN424 is an orally active and selective GPR6 inverse agonist with a Ki of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.70%
- CAS. Nr.: 2254706-21-1
- Formel: C24H29F2N5O3
- Molecular Weight:473.52
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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GPCR/G Protein Compound Library
HY-L006
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Clinical Compound Library
HY-L026
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Drug Repurposing Compound Library
HY-L035
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Orally Active Compound Library
HY-L061
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Anti-Parkinson's Disease Compound Library
HY-L085
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Neurodegenerative Disease-related Compound Library
HY-L086
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
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Bioactive Compound Library Max
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Publications Citing Use of MedChemExpress (MCE) Solangepras
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Biologische Aktivität
CVN424 (Compound 6i) has 265 fold and 68 fold selectivities over GPR3 and GPR12[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2254706-21-1
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Appearance Solid
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Molecular Weight 473.52
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Formel C24H29F2N5O3
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Color Light yellow to green yellow
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SMILES
FC1=C(OC2CCN(C3=NC4=C(N=C3N[C@H]5COCC5)CN(CC4)C(C)=O)CC2)C=CC(F)=C1
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Synonyms
CVN424
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Med Chem
Development of Fluorescent AF64394 Analogues Enables Real-Time Binding Studies for the Orphan Class A GPCR GPR3. [Abstract]2023 Nov 9;66(21):15025-15041. PMID: 37907069
Lösungsmittel & Löslichkeit
DMSO : 58.33 mg/mL (123.18 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Huikai Sun, et al. First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate. J Med Chem. 2021 Apr 16. [Content Brief]
[2]. Nicola L Brice, et al. Development of CVN424: A Selective and Novel GPR6 Inverse Agonist Effective in Models of Parkinson Disease. J Pharmacol Exp Ther. 2021 Jun;377(3):407-416. [Content Brief]
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 |
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| DMSO | 1 mM | 2.1118 mL | 10.5592 mL | 21.1184 mL | 52.7961 mL |
| 5 mM | 0.4224 mL | 2.1118 mL | 4.2237 mL | 10.5592 mL | |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1118 mL | 5.2796 mL | |
| 15 mM | 0.1408 mL | 0.7039 mL | 1.4079 mL | 3.5197 mL | |
| 20 mM | 0.1056 mL | 0.5280 mL | 1.0559 mL | 2.6398 mL | |
| 25 mM | 0.0845 mL | 0.4224 mL | 0.8447 mL | 2.1118 mL | |
| 30 mM | 0.0704 mL | 0.3520 mL | 0.7039 mL | 1.7599 mL | |
| 40 mM | 0.0528 mL | 0.2640 mL | 0.5280 mL | 1.3199 mL | |
| 50 mM | 0.0422 mL | 0.2112 mL | 0.4224 mL | 1.0559 mL | |
| 60 mM | 0.0352 mL | 0.1760 mL | 0.3520 mL | 0.8799 mL | |
| 80 mM | 0.0264 mL | 0.1320 mL | 0.2640 mL | 0.6600 mL | |
| 100 mM | 0.0211 mL | 0.1056 mL | 0.2112 mL | 0.5280 mL |
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