Tavapadon (DC11103) chemical structure
Chemical structureResearch use only
CAT. NO. DC11103Featured

Tavapadon

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Product overview

Description & Application

Tavapadon (PF-06649751) is a non-catechol D1/D5 partial agonist for dopamine-receptor and motor-function research.

ParameterValue
Chemical NameTavapadon
CAS No.1643489-24-0
SynonymsTavapadon; (Rac)-Tavapadon; PT4P8MJP8L; Tavapadon (USAN); Tavapadon [USAN]; BCP32804; DB14899; D11431; (-)-1,5-dimethyl-6-(2-methyl-4-((3-(trifluoromethyl)pyridin-2-yl)oxy)phenyl)-2,4(1H,3H)-pyrimidinedione; 2,4(1H,3H)-Pyrimidinedione, 1,5-dimethyl-6-(2-methyl-4-((3-(trifluoromethyl)-2-pyridinyl)oxy)phenyl)-, (-)-; 1,5-dimethyl-6-[2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]oxyphenyl]pyrimidine-2,4-dione; DA-67955; PF-06649751; GTPL13372; UNII-PT4P8MJP8L; CVL-751; 1,5-dimethyl-6-(2-methyl-4-{[3-(trifluoromethyl)pyridin-2-yl]oxy}phenyl)-3H-pyrimidine-2,4-dione; AC-36997; AKOS040742684; CS-0131271; 1,5-dimethyl-6-[2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]oxy-phenyl]pyrimidine-2,4-dione; AKQXQLUNFKDZBN-UHFFFAOYSA-N; 1643462-64-9; SCHEMBL16334991; DTXSID301337071; tavapadonum; 1,5-dimethyl-6-[2-methyl-4-[[3-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]-2,4(1H,3H)-pyrimidinedione; 1,5-dimethyl-6-(2-methyl-4-((3-(trifluoromethyl)pyridin-2-yl)oxy)phenyl)-1,2,3,4-tetrahydropyrimidine-2,4-dione; 1,5-Dimethyl-6-(2-methyl-4-((3-(trifluoromethyl)pyridin-2-yl)oxy)phenyl)pyrimidine-2,4(1H,3H)-dione; 1,5-dimethyl-6-(2-methyl-4-{[3-(trifluoromethyl)pyridin-2-yl]oxy}phenyl)-1,2,3,4-tetrahydropyrimidine-2,4-dione; Tavapadon?; DB-186035; 1643489-24-0; G17190; 6-(4-(3-(Trifluoromethyl)pyridin-2-yloxy)-2-methylphenyl)-1,5-dimethylpyrimidine-2,4(1h,3h)-dione; Tavapadon (USAN/INN); PF 06649751; PF-6649751; PF06649751; HY-119486A; 86W; TAVAPADON [INN]; (-)-1,5-DIMETHYL-6-(2-METHYL-4-((3-(TRIFLUOROMETHYL)-2-PYRIDINYL)OXY)PHENYL)-2,4(1H,3H)-PYRIMIDINEDIONE; CHEMBL3697617; (-)-1,5-Dimethyl-6-(2-methyl-4-((3-(trifluoromethyl)pyridin-2-yl)oxy)phenyl)pyrimidine-2,4(1H,3H)-dione; EX-A3416; MS-26523
FormulaC19H16F3N3O3
M.Wt391.343854904175
SMILESFC(C1=CC=CN=C1OC1C=CC(=C(C)C=1)C1=C(C)C(NC(N1C)=O)=O)(F)F
Purity98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Dopamine D1 / D5 · Literature evidence

Biological Activity

Tavapadon (PF-06649751) is a non-catechol D1/D5 partial agonist for dopamine-receptor and motor-function research. Published human study results are separated from preclinical assays below.

In Vitro

No separate compound-specific cell or biochemical result is available from the sources summarized here.

In Vivo

No compound-specific animal efficacy result is established by the sources summarized here.

Clinical / Human Evidence

EndpointModel / conditions / sourceReported result
Trial populationRandomized phase II study in early Parkinson disease; 57 participants, 15 weeks. [1]29 received PF-06649751 (tavapadon) and 28 placebo; 47 completed the study.
Study exposureOnce-daily oral treatment, individually titrated from 0.25 mg to a permitted maximum of 15 mg. [1]Doses were optimized for tolerability and motor-symptom control; this describes the trial rather than a recommended regimen.
Motor endpointMDS-UPDRS part III at week 15. [1]Mean change was −9.0 versus −4.3 with placebo; reported between-group difference 4.8 points, 90% CI 1.0–8.6, p=0.0407.
Adverse events and limitationPhase II safety observations. [1]Nausea, headache, dry mouth, somnolence and tremor were reported, mostly mild or moderate. The trial stopped enrollment early for reasons unrelated to its results.

Interpretation

These results concern a clinical investigational formulation, not administration of the supplied research reagent.

Original studies

References

  1. Riesenberg R, et al. PF-06649751 efficacy and safety in early Parkinson's disease: a randomized, placebo-controlled trial. Therapeutic advances in neurological disorders (2020).

Product documentation

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

For additional quantities or product documentation, contact info@dcchemicals.com.

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