Tavapadon
Based on 3 publication(s) in Google Scholar
Tavapadon (PF-06649751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease.
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- Pureza: 99.94%
- No. CAS: 1643489-24-0
- Fòrmula: C19H16F3N3O3
- Peso molecular:391.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) Tavapadon
MoreVer todos los productos específicos de isoformas Dopamine Receptor
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Actividad biológica
dopamine D1/D5 receptor[1]
Tavapadon (0.04 mg/kg, s.c.) also improves parkinsonian disability scores with the maximal improvement observed at 110 min after drug administration[1].
Higher doses of Tavapadon (0.1 and 0.15 mg/kg; s.c.) leads to statistically significant improvement relative to vehicle in locomotor activity[1].
Tavapadon (0.1 mg/kg; s.c.) has the mean maximal unbound plasma concentration of 8 nM and achieves 3 hours after compound administration in captive-bred macaques[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1643489-24-0
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Appearance Solid
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Peso molecular 391.34
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Fòrmula C19H16F3N3O3
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Color White to light brown
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SMILES
O=C1NC(C(C)=C(C2=CC=C(OC3=NC=CC=C3C(F)(F)F)C=C2C)N1C)=O
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Synonyms
PF-06649751; CVL-751
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Targeting dopamine transporter for treating social transmission of depression-like behaviors in male mice. [Abstract]2026 Jun 16. PMID: 42303982 -
Nat Commun
2022 Jun 8;13(1):3186. PMID: 35676276 -
ACS Chem Neurosci
Estimation of Dopamine D1 Receptor Agonist Binding Kinetics Using Time-Resolved Functional Assays: Relation to Agonist-Induced Receptor Internalization by Investigational Antiparkinsonian Therapeutics. [Abstract]2025 Jul 2;16(13):2502-2512. PMID: 40537032
Solvente y solubilidad
DMSO : 66.67 mg/mL (170.36 mM; ultrasonic and warming and heat to 60°C; 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.
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (481 KB)
- English - EN (481 KB)
- Français - FR (481 KB)
- Deutsch - DE (481 KB)
- Norwegian - NO (481 KB)
- Español - ES (481 KB)
- Swedish - SV (481 KB)
- Italian - IT (481 KB)
- Korean - KR (481 KB)
- Portuguese - PT (481 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.5553 mL | 12.7766 mL | 25.5532 mL | 63.8831 mL |
| 5 mM | 0.5111 mL | 2.5553 mL | 5.1106 mL | 12.7766 mL | |
| 10 mM | 0.2555 mL | 1.2777 mL | 2.5553 mL | 6.3883 mL | |
| 15 mM | 0.1704 mL | 0.8518 mL | 1.7035 mL | 4.2589 mL | |
| 20 mM | 0.1278 mL | 0.6388 mL | 1.2777 mL | 3.1942 mL | |
| 25 mM | 0.1022 mL | 0.5111 mL | 1.0221 mL | 2.5553 mL | |
| 30 mM | 0.0852 mL | 0.4259 mL | 0.8518 mL | 2.1294 mL | |
| 40 mM | 0.0639 mL | 0.3194 mL | 0.6388 mL | 1.5971 mL | |
| 50 mM | 0.0511 mL | 0.2555 mL | 0.5111 mL | 1.2777 mL | |
| 60 mM | 0.0426 mL | 0.2129 mL | 0.4259 mL | 1.0647 mL | |
| 80 mM | 0.0319 mL | 0.1597 mL | 0.3194 mL | 0.7985 mL | |
| 100 mM | 0.0256 mL | 0.1278 mL | 0.2555 mL | 0.6388 mL |
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