| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
dopamine D1/D5 receptor
Tavapadon targets dopamine D1 and D5 receptors with Ki values of 9 nM and 13 nM, respectively. It acts as a selective partial agonist at these receptors with minimal to no activity at D2, D3, and D4 receptors. It stimulates the Gs/Gaolf pathway, leading to an increase in intracellular cyclic AMP (cAMP). |
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| ln Vitro |
Tavapadon has Ki values of 9 nM for D1 and 13 nM for D5 receptors. It shows high affinity and selectivity for D1 and D5 receptors with significantly lower affinity for D2, D3, and D4 receptors. Its unique pharmacological profile is characterized by partial agonism at D1/D5 receptors.
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| ln Vivo |
Tavapadon (PF-06649751; 0.02 and 0.04 mg/kg; s.c.) has little to no effect on locomotor activity when administered at the 0.04 mg/kg test dose, in contrast to the 0.02 mg/kg dose[1].
Tavapadon (0.04 mg/kg, s.c.) also reduces parkinsonian disability scores; the greatest reduction in disability was seen 110 minutes after the drug was administered[1]. Increased Tavapadon dosages (0.1 and 0.15 mg/kg; s.c.) result in a statistically significant improvement in locomotor activity when compared to a vehicle[1]. Tavapadon (0.1 mg/kg; s.c.) in captive-bred macaques results in a mean maximal unbound plasma concentration of 8 nM three hours after compound administration[1]. In vivo, tavapadon aims to provide efficacy comparable to levodopa with a reduced risk of dyskinesia and other motor complications. Preclinical studies in various animal models, including rodents and non-human primates, have demonstrated its potential in improving motor function. It is being developed for the treatment of Parkinson's disease. |
| Enzyme Assay |
In vitro receptor binding assays for tavapadon measure its affinity for dopamine D1 and D5 receptors using radioligand displacement techniques, with Ki values of 9 nM and 13 nM, respectively. Selectivity over D2, D3, and D4 receptors is confirmed by testing against these subtypes. Functional assays measure cAMP accumulation as a readout of receptor activation.
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| Cell Assay |
In vitro cell-based assays for tavapadon use cells expressing dopamine D1 and D5 receptors. Cells are treated with serial dilutions of the compound, and cAMP accumulation is measured by ELISA or other immunoassay methods. The EC50 for receptor activation is calculated from dose-response curves. Selectivity over other dopamine receptor subtypes is confirmed in parallel assays.
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| Animal Protocol |
In vivo animal models for tavapadon include rodent and non-human primate models of Parkinson's disease. Motor function is assessed using behavioral tests such as the rotarod test or open field test. The compound's effects on motor improvement and dyskinesia are evaluated. Pharmacodynamic studies measure D1/D5 receptor occupancy in the brain.
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| ADME/Pharmacokinetics |
Tavapadon has a molecular formula of C₁₉H₁₆F₃N₃O₃ and a molecular weight of 391.34 g/mol. It is orally administered. It is also known as PF-6649751, CVL-751, and PF-06649751. The compound is stored under appropriate conditions for research use.
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| Toxicity/Toxicokinetics |
The toxicity profile of tavapadon is characterized in preclinical safety studies. As a dopamine D1/D5 receptor partial agonist, it is generally well-tolerated at therapeutic doses. Common adverse effects may include those associated with dopaminergic stimulation. The compound is for research use only and is not approved for clinical use.
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| References | |
| Additional Infomation |
Tavapadon is currently being investigated in the clinical trial NCT02262767 (a study of the safety, tolerability, and pharmacokinetics of PF-06649751 in combination with trimetobenzamide hydrochloride in healthy subjects).
Drug Indication Treatment of Parkinson's Disease Tavapadon (PF-6649751, CVL-751) is a first-in-class, orally administered selective partial agonist for dopamine D1 and D5 receptors. It has Ki values of 9 nM and 13 nM for D1 and D5, respectively. It has been investigated for the treatment of Parkinson's disease. Tavapadon aims to provide efficacy comparable to levodopa with reduced dyskinesia risk. |
| Molecular Formula |
C19H16F3N3O3
|
|---|---|
| Molecular Weight |
391.343854904175
|
| Exact Mass |
391.114
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| Elemental Analysis |
C, 58.31; H, 4.12; F, 14.56; N, 10.74; O, 12.26
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| CAS # |
1643489-24-0
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| Related CAS # |
(Rac)-Tavapadon; 1643462-64-9
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| PubChem CID |
86764100
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| Appearance |
Solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.549
|
| LogP |
3.66
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
665
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC(C1=CC=CN=C1OC1C=CC(=C(C)C=1)C1=C(C)C(NC(N1C)=O)=O)(F)F
|
| InChi Key |
AKQXQLUNFKDZBN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H16F3N3O3/c1-10-9-12(28-17-14(19(20,21)22)5-4-8-23-17)6-7-13(10)15-11(2)16(26)24-18(27)25(15)3/h4-9H,1-3H3,(H,24,26,27)
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| Chemical Name |
1,5-dimethyl-6-[2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]oxyphenyl]pyrimidine-2,4-dione
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| Synonyms |
CVL-751; CVL 751; CVL751; PF-6649751; PF 6649751; PF6649751
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~255.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.39 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5553 mL | 12.7766 mL | 25.5532 mL | |
| 5 mM | 0.5111 mL | 2.5553 mL | 5.1106 mL | |
| 10 mM | 0.2555 mL | 1.2777 mL | 2.5553 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT07158827
Conditions:Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT04760769
Conditions:Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT04223193
Conditions:Parkinson Disease
Title:Fixed-Dose Trial in Early Parkinson's Disease (PD)
Status:Completed
updateDate:2025-07-28
Ctid:NCT04201093
Link: https://clinicaltrials.gov/ct2/show/NCT04201093
Conditions:Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT06895356
Conditions:Healthy VolunteerLink: https://clinicaltrials.gov/ct2/show/NCT04542499
Conditions:Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT05404542
Conditions:Renal ImpairmentLink: https://clinicaltrials.gov/ct2/show/NCT05610189
Conditions:Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT02373072
Conditions:Idiopathic Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT05404529
Conditions:Hepatic ImpairmentLink: https://clinicaltrials.gov/ct2/show/NCT05581823
Conditions:Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT04295642
Conditions:Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT02847650
Conditions:Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT02687542
Conditions:Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT04241393
Conditions:Healthy SubjectsLink: https://clinicaltrials.gov/ct2/show/NCT03185481
Conditions:Parkinson's Disease With Motor FluctuationsLink: https://clinicaltrials.gov/ct2/show/NCT02224664
Conditions:Parkinson's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT02066909
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT02262767
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT01981694
Conditions:HealthyLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2015-004912-39
Condition:Parkinson's DiseaseParkinson KrankheitProducts are for research use only; We do not sell to patients
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