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Cat. No.: HY-175001

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D1/D5 Receptor agonist-1

D1/D5 Receptor agonist-1 is a highly brain-penetrant and orally active D1/D5 receptor agonist. D1/D5 Receptor agonist-1 maintains considerable efficacy in the cAMP pathway and in β-arrestin recruitment, with EC₅₀s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a K_i of 111 nM (D1R binding affinity). D1/D5 Receptor agonist-1 inhibits β-arrestin signaling in a rat with L-DOPA (HY-N0304) induced dyskinesias. D1/D5 Receptor agonist-1 can be used for the study of Parkinson’s disease.

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

Formula: C₁₈H₁₃FN₄O₄
Molecular Weight:368.32

Storage:

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

Data Sheet (275 KB)

D1/D5 Receptor agonist-1 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target^[1]

D₁ Receptor

D₅ Receptor

All Dopamine Receptor Isoforms :

All Arrestin Isoforms :

In Vitro

D1/D5 Receptor agonist-1 (Compound 24) (10^-4-10 μM) maintains considerable efficacy in the cAMP pathway and in β-arrestin recruitment, with EC₅₀s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a K_i of 111 nM (D1R binding affinity)^[1].

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

Parmacokinetics

Species	Dose	Route	CL	T_1/2	V_ss	AUC	F
Rat^[1]	1 mg/kg	i.v.	2.55 mL/min/kg	2.32 h	0.50 L/kg	/	/
Rat^[1]	5 mg/kg	p.o.	/	/	/	6450 ng·h/mL	92.5 %

In Vivo

D1/D5 Receptor agonist-1 (Compound 24) (0.3-3 mg/kg, p.o., single dose) inhibits β-arrestin signaling in a rat model of Parkinson’s disease with L-DOPA (HY-N0304)-induced dyskinesias^[1].

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

Animal Model:

6-OHDA and L-DOPA (HY-N0304)-induced dyskinesias in adult male SD rats (180 g)^[1]
Dosage:

0.3, 1, 3 mg/kg
Administration:

p.o. for a single dose
Result:

Decreased EEG beta power over a longer time course (up to 4 h).
Showed comparable efficacy to a therapeutic dose of L-DOPA and with significantly fewer concomitant dyskinesias at doses with predicted D1 RO of 30 to 50%.

Chemical Information

Molecular Weight 368.32
Formula C₁₈H₁₃FN₄O₄
SMILES

FC1=C(C2=C(C)C(NC(N2C)=O)=O)N=CC(OC3=C(C=CO4)C4=CC=N3)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 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)

References

[1]. Rodríguez Sarmiento RM, et al. Orally Bioavailable Dopamine D1/D5 Receptor-Biased Agonists to Study the Role of β-Arrestin in Treatment-Related Dyskinesia in Parkinson's Disease. J Med Chem. 2025 Jul 10;68(13):13532-13561. [Content Brief]

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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.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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D1/D5 Receptor agonist-1

All Dopamine Receptor Isoforms

All Arrestin Isoforms