| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
D4 Receptor
ABT-724 trihydrochloride targets the dopamine D4 receptor as a potent and highly selective agonist. It has an EC50 of 12.4 nM for the human dopamine D4 receptor and functions as a partial agonist at the rat D4 receptor with an EC50 of 14.3 nM. It displays no agonist activity at D2 receptors (EC50 > 10 μM). |
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| ln Vitro |
ABT-724 displays a selective biochemical profile, as demonstrated by its lack of binding affinity for over 70 neurotransmitter/uptake/ion channels, such as D2, D3, or D5 receptors, at concentrations up to 10 μM. There's a low affinity (Ki = 2780 nM) for 5-HT1A receptors. At concentrations of 10 μM, ABT-724 does not inhibit PDE activity of PDE1, PDE5, or PDE6[1].
In vitro, ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for the human receptor. It functions as a partial agonist at the rat D4 receptor with an EC50 of 14.3 nM. It displays no agonist activity at D2 receptors. |
| ln Vivo |
ABT-724 (8.8 μg/kg; subcutaneous injection; daily; for 5 days; male adult Wistar rats) treatment dose-dependently promotes penile erection when administered subcutaneously to conscious rats[1].
In vivo, ABT-724 trihydrochloride was created as a potential medication to treat erectile dysfunction. As a selective D4 agonist, it can be administered to animal models to study the role of D4 receptors in sexual function, cognition, and other physiological processes. Its in vivo efficacy has been demonstrated in preclinical models. |
| Enzyme Assay |
In vitro receptor binding assays for ABT-724 trihydrochloride involve measuring its affinity for dopamine D4 and D2 receptors. Radioligand binding studies using ³H-spiperone or other dopamine ligands are performed on membranes from cells expressing the receptors. Functional assays measure its ability to activate D4 receptor-mediated signaling, such as calcium influx or GTPγS binding.
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| Cell Assay |
For in vitro cell-based assays, cells expressing dopamine D4 receptors (e.g., HEK-293 cells co-transfected with a G protein) are cultured and treated with ABT-724 trihydrochloride at various concentrations. Receptor activation is measured by quantifying calcium influx using fluorescent calcium indicators or by measuring GTPγS binding. Cell viability is assessed by standard assays.
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| Animal Protocol |
Male adult Wistar rats (~300 g)
8.8 μg/kg Subcutaneous injection; daily; for 5 days In vivo animal studies with ABT-724 trihydrochloride are conducted in models of erectile dysfunction and other D4-mediated conditions. The compound is administered orally or intraperitoneally to rodents. Erectile function is assessed by measuring intracavernosal pressure. Its effects on cognition and behavior can be evaluated using appropriate behavioral tests. |
| ADME/Pharmacokinetics |
ABT-724 trihydrochloride (CAS: 587870-77-7) has a molecular weight of 389.75 g/mol and a molecular formula of C14H21ClN4·3HCl. Appearance: solid powder. Purity: ≥98%. Solubility: DMSO. Storage: -20°C. The compound is a potent and highly selective dopamine D4 receptor agonist.
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| Toxicity/Toxicokinetics |
ABT-724 trihydrochloride is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a D4 receptor agonist, it may have effects on sexual function, cognition, and behavior. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for the human receptor. It was developed as a potential treatment for erectile dysfunction. It is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C₁₇H₂₂CL₃N₅
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|---|---|
| Molecular Weight |
402.749080181122
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| Exact Mass |
401.094
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| Elemental Analysis |
C, 50.70; H, 5.51; Cl, 26.41; N, 17.39
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| CAS # |
587870-77-7
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| Related CAS # |
ABT-724; 70006-24-5
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| PubChem CID |
16759165
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
355
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.Cl.Cl.C1=CC=C(N2CCN(CC3=NC4=CC=CC=C4N3)CC2)N=C1
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| InChi Key |
AZFUVPBLKQGSRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H19N5.3ClH/c1-2-6-15-14(5-1)19-16(20-15)13-21-9-11-22(12-10-21)17-7-3-4-8-18-17;;;/h1-8H,9-13H2,(H,19,20);3*1H
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| Chemical Name |
2-[(4-pyridin-2-ylpiperazin-1-yl)methyl]-1H-benzimidazole;trihydrochloride
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| Synonyms |
ABT-724 trihydrochloride; ABT724 triHCl; ABT 724 hydrochloride; ABT-724 (3HCl)
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ≥ 100 mg/mL (~248.3 mM)
DMSO: ~20 mg/mL (~49.7 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (248.29 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4829 mL | 12.4146 mL | 24.8293 mL | |
| 5 mM | 0.4966 mL | 2.4829 mL | 4.9659 mL | |
| 10 mM | 0.2483 mL | 1.2415 mL | 2.4829 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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