1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
  3. (Rac)-Tavapadon

(Rac)-Tavapadon (Synonyms: (Rac)-PF-06649751; (Rac)-CVL-751)

Cat. No.: HY-119486A
Handling Instructions

(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity.

For research use only. We do not sell to patients.

(Rac)-Tavapadon Chemical Structure

(Rac)-Tavapadon Chemical Structure

CAS No. : 1643462-64-9

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10 mM * 1  mL in DMSO USD 165 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity[1].

IC50 & Target[1]

D1 Receptor

 

In Vitro

(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751; compound 32) has EMAXs of 118% and 30% in the GS activation assay and the β-arrestin2 recruitment assay[1].

Molecular Weight

391.34

Formula

C₁₉H₁₆F₃N₃O₃

CAS No.

1643462-64-9

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (106.48 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 4.17 mg/mL (10.66 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

(Rac)-Tavapadon(Rac)-PF-06649751(Rac)-CVL-751Dopamine ReceptorGSactivatioβ-arrestin2recruitmentGS-cAMPantiparkinsonianParkinson’sDiseaseInhibitorinhibitorinhibit

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(Rac)-Tavapadon
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