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Cat. No.: 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.

For research use only. We do not sell to patients.

CAS No.: 2648548-71-2
Formula: 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 No.: 2648548-71-2

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

Biological Activity
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- In Vitro
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Biological Activity

Description

IC₅₀ & Target

^[1]

D₃ Receptor

D₂ Receptor

All Dopamine Receptor Isoforms :

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 No. 2648548-71-2
Molecular Weight 451.53
Formula 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
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Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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.

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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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Biological Activity
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- In Vitro
Chemical Information
Purity & Documentation
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EA-RK-110

All Dopamine Receptor Isoforms

Biological Activity

Description

IC50 & Target

In Vitro

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EA-RK-110 Related Classifications

HY-189717 Related Classifications

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