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

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

Cat. No.: HY-119486A Purity: 99.87%
COA Handling Instructions

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(Rac)-Tavapadon ((Rac)-PF-06649751) 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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 149 In-stock
Solution
10 mM * 1 mL in DMSO USD 149 In-stock
Solid
5 mg USD 135 In-stock
10 mg USD 220 In-stock
50 mg USD 600 In-stock
100 mg USD 945 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of (Rac)-Tavapadon:

(Rac)-Tavapadon Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(Rac)-Tavapadon Related Antibodies
Clinical Trial
Molecular Weight

391.34

Formula

C19H16F3N3O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (106.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5553 mL 12.7766 mL 25.5532 mL 63.8831 mL
5 mM 0.5111 mL 2.5553 mL 5.1106 mL 12.7766 mL
10 mM 0.2555 mL 1.2777 mL 2.5553 mL 6.3883 mL
15 mM 0.1704 mL 0.8518 mL 1.7035 mL 4.2589 mL
20 mM 0.1278 mL 0.6388 mL 1.2777 mL 3.1942 mL
25 mM 0.1022 mL 0.5111 mL 1.0221 mL 2.5553 mL
30 mM 0.0852 mL 0.4259 mL 0.8518 mL 2.1294 mL
40 mM 0.0639 mL 0.3194 mL 0.6388 mL 1.5971 mL
50 mM 0.0511 mL 0.2555 mL 0.5111 mL 1.2777 mL
60 mM 0.0426 mL 0.2129 mL 0.4259 mL 1.0647 mL
80 mM 0.0319 mL 0.1597 mL 0.3194 mL 0.7985 mL
100 mM 0.0256 mL 0.1278 mL 0.2555 mL 0.6388 mL
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(Rac)-Tavapadon Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(Rac)-Tavapadon1643462-64-9(Rac)-PF-06649751 (Rac)-CVL-751Dopamine ReceptorArrestinGSactivatioβ-arrestin2recruitmentGS-cAMPantiparkinsonianParkinson’sDiseaseInhibitorinhibitorinhibit

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