(Rac)-Tavapadon
Based on 1 Customer Validation
(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity.
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- Pureté : 99.49%
- CAS No.: 1643462-64-9
- Formule: C19H16F3N3O3
- Masse moléculaire:391.34
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
D1 Receptor |
In Vitro
(Rac)-Tavapadon ((Rac)-PF-06649751; compound 32) has EMAXs of 118% and 30% in the GS activation assay and the β-arrestin2 recruitment assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1643462-64-9
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Appearance Solid
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Masse moléculaire 391.34
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Formule C19H16F3N3O3
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Color White to off-white
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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
(Rac)-PF-06649751; (Rac)-CVL-751
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
In Vitro:
DMSO : 41.67 mg/mL (106.48 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| 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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