Art. -Nr.: HY-119943

PF-06256142

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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

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Reinheit: 99.90%
CAS. Nr.: 1609583-14-3
Formel: C₂₁H₁₆N₄O₂
Molecular Weight:356.38

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-06256142 Chemical Structure

CAS. Nr.: 1609583-14-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Human D₁ Receptor

33 nM (EC₅₀)

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	11 nM Compound: 6; PF6142	Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay	[PMID: 31098001]
HEK293	EC₅₀	320 nM Compound: 6; PF6142	Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay	[PMID: 31098001]

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 K_i of 4.8 nM for D5 exquisitely selective than D2 (K_i>10 μM)^[1].

MedChemExpress (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].

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%), T_1/2 (2.3 h).

Chemical Information

CAS. Nr. 1609583-14-3
Appearance Solid
Molecular Weight 356.38
Formel C₂₁H₁₆N₄O₂
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

Neuron

Structural basis of psychedelic LSD recognition at dopamine D1 receptor. [Abstract]

2024 Jul 25:S0896-6273(24)00494-X. PMID: 39094559

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8060 mL

14.0300 mL

28.0599 mL

5 mM

0.5612 mL

2.8060 mL

5.6120 mL

10 mM

0.2806 mL

1.4030 mL

2.8060 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Davoren JE, et al. Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. J Med Chem. 2018 Nov 15. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

PF-06256142

1 Cited Publications

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PF-06256142

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Neurotransmitter Receptor Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Antidepressant Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Dopamine Receptor Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-06256142

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-06256142

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Neurotransmitter Receptor Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Antidepressant Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Dopamine Receptor Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-06256142

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-06256142 Related Classifications

HY-119943 Related Classifications