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Art. -Nr.: HY-189717

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EA-RK-110

EA-RK-110 is a dopamine D3 receptor inverse agonist derived from Cariprazine (HY-14763) that stabilizes the inactive conformation and attenuates G protein signaling. EA-RK-110 weakly activates dopamine D2 receptor-mediated signaling. EA-RK-110 mediates inverse agonism through its meta-nitrile group via receptor residue interactions and toggle-switch modulation. EA-RK-110 can be used for research on dopamine receptor-related diseases.

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CAS. Nr.: 2648548-71-2
Formel: C₂₃H₃₂F₃N₅O
Molecular Weight:451.53

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

EA-RK-110 Chemical Structure

CAS. Nr.: 2648548-71-2

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Use of MCE Products

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

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^[1]

D₃ Receptor

D₂ Receptor

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In Vitro

EA-RK-110 acts as a D3R inverse agonist in BRET G protein activation/profiling assays in HEK293T cells, and its inverse agonism is converted to weak partial agonism by S192A/H349A and enhanced by Y373F^[1].
EA-RK-110 is a weak D2R partial agonist in cell-based BRET assays^[1].

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

Chemical Information

CAS. Nr. 2648548-71-2
Molecular Weight 451.53
Formel C₂₃H₃₂F₃N₅O
SMILES

CN(C)C(N[C@@H](CC1)CC[C@H]1CCN(CC2)CCN2C3=CC(C#N)=CC(C(F)(F)F)=C3)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Hadas Yardeni E, et al. The structure of the dopamine D3 receptor bound to cariprazine reveals principles for partial agonists with designed pharmacology. Sci Adv. 2026 Aug 28;12(35):eaef7411.

Calculators

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)}

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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.

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EA-RK-110

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

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IC50 & Target

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HY-189717 Related Classifications

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