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

PF-06256142 

Cat. No.: HY-119943 Purity: 98.70% ee.: 100.00%
Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 440 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3400 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PF-06256142:

Top Publications Citing Use of Products
  • 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].

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

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].

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

388.44

Formula

C21H16N4O2S

CAS No.
SMILES

CC1=[[email protected]]([[email protected]]2=C(C)N=CC3=NC=CN32)C=CC(OC4=C(C=CO5)C5=CC=N4)=C1.[S]

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 (514.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5744 mL 12.8720 mL 25.7440 mL
5 mM 0.5149 mL 2.5744 mL 5.1488 mL
10 mM 0.2574 mL 1.2872 mL 2.5744 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (12.87 mM); Clear solution

  • 2.

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

    Solubility: ≥ 5 mg/mL (12.87 mM); Clear solution

  • 3.

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

    Solubility: ≥ 5 mg/mL (12.87 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PF-06256142
Cat. No.:
HY-119943
Quantity:
MCE Japan Authorized Agent: