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

PF-06256142 

Cat. No.: HY-119943
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

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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-lives (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.

1609583-14-3

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

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

References
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Keywords:

PF-06256142PF06256142PF 06256142Dopamine ReceptordopaminereceptorsParkinson'sdiseaseschizophreniaInhibitorinhibitorinhibit

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PF-06256142
Cat. No.:
HY-119943
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