1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. ABT-724

ABT-724, a chemical probe, is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.

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

ABT-724

ABT-724 Chemical Structure

CAS No. : 70006-24-5

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Description

ABT-724, a chemical probe, is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].

IC50 & Target

D4 Receptor

 

D5 Receptor

 

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
12.4 nM
Compound: 1 (ABT-724)
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
12.4 nM
Compound: 1a, ABT-724
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
12.4 nM
Compound: 3a
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
[PMID: 15084133]
HEK293 EC50
13.7 nM
Compound: 1a, ABT-724
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
14.3 nM
Compound: 1 (ABT-724)
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
23.2 nM
Compound: 1 (ABT-724)
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
[PMID: 15239663]
In Vitro

ABT-724 exhibits a selective biochemical profile, as indicates by a lack of binding affinity for >70 neurotransmitter/uptake/ion channels including D2, D3, or D5 receptors up to a 10 μM concentration. A weak affinity to 5-HT1A receptors (Ki = 2780 nM) is observed. ABT-724 does not inhibit the PDE activity of PDE1, PDE5, or PDE6 at 10 μM concentrations[1].

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

In Vivo

ABT-724 (8.8 μg/kg; subcutaneous injection; daily; for 5 days; male adult Wistar rats) treatment dose-dependently facilitates penile erection when given s.c. to conscious rats[1].

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

Animal Model: Male adult Wistar rats (~300 g)[1]
Dosage: 8.8 μg/kg
Administration: Subcutaneous injection; daily; for 5 days
Result: Dose-dependently facilitated penile erection.
Molecular Weight

293.37

Formula

C17H19N5

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

C1(NC(CN2CCN(C3=NC=CC=C3)CC2)=N4)=C4C=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 4.17 mg/mL (14.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4087 mL 17.0433 mL 34.0866 mL
5 mM 0.6817 mL 3.4087 mL 6.8173 mL
View the Complete Stock Solution Preparation Table

* 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.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4087 mL 17.0433 mL 34.0866 mL 85.2166 mL
5 mM 0.6817 mL 3.4087 mL 6.8173 mL 17.0433 mL
10 mM 0.3409 mL 1.7043 mL 3.4087 mL 8.5217 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
ABT-724
Cat. No.:
HY-14330
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