PF-4211
PF-4211 is a selective non-catechol D1R agonist with a Ki value of 2.2 μM.. PF-4211 activates adenylate cyclase by binding to D1R, thereby increasing intracellular cAMP levels. PF-4211 can be used in research related to Parkinson's disease and schizophrenia.
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- CAS No.: 2292115-41-2
- Formule: C17H13N3O2
- Masse moléculaire:291.30
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[2]|
Human D1 Receptor 2519 nM (EC50) |
In Vitro
PF-4211 (Compound 6) acts as a partial agonist at the hD1 receptor in HEK293 cells overexpressing hD1, with a geometric mean functional EC50 of 2.293 μM and 37% maximal effect relative to dopamine[1].
PF-4211 binds directly to the hD1 receptor with a geometric mean binding Ki of 2.2 μM[1].
PF-4211 (11-point concentration response curve with half-log increments; 30 min) acts as a partial agonist at human D1 receptors expressed in HEK293 cells, with an EC50 of 2519 nM and a maximum efficacy of 42% relative to dopamine[2].
PF-4211 (10-10-10-4 M; 30 min) induces a dose-dependent increase in cAMP in hD1R-expressing HEK293 cells, with a lower maximum efficacy than dopamine and optimized non-catechol analogs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2292115-41-2
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Masse moléculaire 291.30
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Formule C17H13N3O2
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SMILES
CN1N=CC=C1C2=CC=C(C=C2)OC3=NC=CC4=C3C=CO4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Davoren JE, et al. Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. Journal of medicinal chemistry. 2018 Dec 27;61(24):11384-11397. [Content Brief]
[2]. Gray DL, et al. Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor. Nature communications. 2018 Feb 14;9(1):674. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-4211 Related Classifications
HY-149168 Related Classifications
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