Tavapadon( PF 6649751 | PF-06649751 )

Catalog No. M12502 CAS No. 1643489-24-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

Tavapadon
Note

Research use only, not for human use.
Brief Description

Tavapadon (PF 6649751, PF-06649751) is an orally available dopamine D1 receptor partial agonist for treatment of Parkinson's disease.
Description

Tavapadon (PF 6649751, PF-06649751) is an orally available dopamine D1 receptor partial agonist for treatment of Parkinson's disease.Parkinson Disease Discontinued.
In Vitro

——
In Vivo

Tavapadon (PF-06649751; 0.02 and 0.04 mg/kg; s.c.) at the 0.04 mg/kg test dose increases locomotor activity, whereas the 0.02 mg/kg dose has little or no effect. Tavapadon (0.04 mg/kg, s.c.) also improves parkinsonian disability scores with the maximal improvement observed at 110 min after drug administration. Higher doses of Tavapadon (0.1 and 0.15 mg/kg; s.c.) leads to statistically significant improvement relative to vehicle in locomotor activity. Tavapadon (0.1 mg/kg; s.c.) has the mean maximal unbound plasma concentration of 8 nM and achieves 3 hours after compound administration in captive-bred macaques.
Synonyms

PF 6649751 | PF-06649751
Pathway

GPCR/G Protein
Target

Dopamine Receptor
Recptor

Dopamine Receptor
Research Area

Neurological Disease
Indication

Parkinson Disease

CAS Number

1643489-24-0
Formula Weight

391.35
Molecular Formula

C19H16F3N3O3
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (255.53 mM)
SMILES

O=C1NC(C(C)=C(C2=CC=C(OC3=NC=CC=C3C(F)(F)F)C=C2C)N1C)=O
Chemical Name

(-)-1,5-Dimethyl-6-[2-methyl-4-[[3-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]-2,4(1H,3H)-pyrimidinedione

1. PCT Int. Appl. (2014), WO 2014207601 A1 20141231.

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