2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. PF-06256142

PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease.

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

PF-06256142 Chemical Structure

PF-06256142 Chemical Structure

CAS No. : 1609583-14-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 440 In-stock
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Solid
5 mg USD 400 In-stock
10 mg USD 680 In-stock
25 mg USD 1350 In-stock
50 mg USD 2200 In-stock
100 mg USD 3400 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PF-06256142:

PF-06256142 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PF-06256142

View All Dopamine Receptor Isoform Specific Products:

View All Isoforms
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease[1].

IC50 & Target[1]

Human D1 Receptor

33 nM (EC50)

In Vitro

PF-06256142 exhibits IC50 values of <5 μM as an antagonist at the following 4 targets: M1 (4.9 μM); CB1 (2.1 μM); H1 (4.6 μM); Nav 1.5 (1.1 μM)[1].
PF-06256142 has an IC50 of approximately 12 μM for hERG[1].
PF-06256142 shows a Ki of 4.8 nM for D5 exquisitely selective than D2 (Ki>10 μM)[1].

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

PF-06256142 Related Antibodies
In Vivo

PF-06256142 exhibits high oral bioavailability (rat 85%) following oral administration (rat 5 mg/kg)[1].
PF-06256142 exhibits terminal elimination half-life (rat 2.3 h) following intravenous administration (rat 5.0 mg/kg)[1].

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

Animal Model: Rat[1]
Dosage: 5.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous injection and oral administration
Result: Oral bioavailability (85%), T1/2 (2.3 h).
Molecular Weight

356.38

Formula

C21H16N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=[C@]([C@]2=C(C)N=CC3=NC=CN32)C=CC(OC4=C(C=CO5)C5=CC=N4)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (561.20 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 2.8060 mL 14.0300 mL 28.0599 mL
5 mM 0.5612 mL 2.8060 mL 5.6120 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (14.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (14.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8060 mL 14.0300 mL 28.0599 mL 70.1498 mL
5 mM 0.5612 mL 2.8060 mL 5.6120 mL 14.0300 mL
10 mM 0.2806 mL 1.4030 mL 2.8060 mL 7.0150 mL
15 mM 0.1871 mL 0.9353 mL 1.8707 mL 4.6767 mL
20 mM 0.1403 mL 0.7015 mL 1.4030 mL 3.5075 mL
25 mM 0.1122 mL 0.5612 mL 1.1224 mL 2.8060 mL
30 mM 0.0935 mL 0.4677 mL 0.9353 mL 2.3383 mL
40 mM 0.0701 mL 0.3507 mL 0.7015 mL 1.7537 mL
50 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4030 mL
60 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1692 mL
80 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8769 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7015 mL
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PF-06256142 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:

PF-062561421609583-14-3PF06256142PF 06256142Dopamine ReceptordopaminereceptorsParkinson'sdiseaseschizophreniaInhibitorinhibitorinhibit

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