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Chemical Structure : Tavapadon
CAS No.: 1643489-24-0
Catalog No.: PC-35468Not For Human Use, Lab Use Only.
Tavapadon (CVL-75, PF-06649751) is a potent, selective orally available dopamine D1/D5 receptor partial agonist with Ki of 9 nM/13 nM, respectively.
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Tavapadon (CVL-75, PF-06649751) is a potent, selective orally available dopamine D1/D5 receptor partial agonist with Ki of 9 nM/13 nM, respectively.
Tavapadon (CVL-75, PF-06649751) shows a low affinity at D2 (Ki ≥ 6210 nM), D3 (Ki ≥ 6720 nM), and D4 (Ki ≥ 4870 nM).
Tavapadon (CVL-75, PF-06649751) acts as a partial agonist by binding at D1 and D5 receptors, corresponding to 65% and 81% of dopamine’s intrinsic activity, respectively, and inducing functional receptor activation, with half-maximal effective concentration (EC50) values of 19 nM and 17 nM.
Tavapadon (CVL-75, PF-06649751) shows potential for the treatment of early through advanced Parkinson's disease (PD), as well as adjunctive therapy in combination with levodopa produce dose-proportional occupancy of D1/D5 receptors.
| M.Wt | 391.35 | |
| Formula | C19H16F3N3O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(-)-1,5-Dimethyl-6-[2-methyl-4-[[3-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]-2,4(1H,3H)-pyrimidinedione |
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1. PCT Int. Appl. (2014), WO 2014207601 A1 20141231.
2. Bezard E, et al. CNS Neurol Disord Drug Targets. 2024;23(4):476-487.
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