Tavapadon (CVL-75, PF-06649751) | Dopamine D1/D5 agonist

Chemical Structure : Tavapadon

CAS No.: 1643489-24-0

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Tavapadon (CVL-751, PF-06649751, PF-6649751)

货号: 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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10 mg	￥2480	In stock
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50 mg	￥7280	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	391.35
分子式	C19H16F3N3O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(-)-1,5-Dimethyl-6-[2-methyl-4-[[3-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]-2,4(1H,3H)-pyrimidinedione

参考文献

1. PCT Int. Appl. (2014), WO 2014207601 A1 20141231.
2. Bezard E, et al. CNS Neurol Disord Drug Targets. 2024;23(4):476-487.

Tavapadon (CVL-751, PF-06649751, PF-6649751)

生物&药学活性

物理化学性质&存储条件

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Tavapadon (CVL-751, PF-06649751, PF-6649751)

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物理化学性质&存储条件

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