ABT 724 trihydrochloride

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Cat.No. 2214 - ABT 724 trihydrochloride | C17H19N5.3HCl | CAS No. 587870-77-7
Description: Potent and selective D4 partial agonist; proerectile
Chemical Name: 2-[[4-(2-Pyridinyl)-1-piperazinyl]methyl]-1H-benzimidazole trihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

Potent dopamine D4 receptor partial agonist (EC50 = 12.4 nM; 61% efficacy vs. dopamine). Has no agonist activity at D2 receptors (EC50 > 10 μM). Selective in rats in vivo; produces penile erection following i.c.v. administration; increases intracavernosal pressure and potentiates the proerectile effects of sildenafil following s.c. administration. Displays minimal side effects.

Technical Data

M. Wt 402.75
Formula C17H19N5.3HCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 587870-77-7
PubChem ID 16759165
InChI Key AZFUVPBLKQGSRI-UHFFFAOYSA-N
Smiles Cl.Cl.Cl.C(N1CCN(CC1)C1=NC=CC=C1)C1=NC2=CC=CC=C2N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 40.27 100

Preparing Stock Solutions

The following data is based on the product molecular weight 402.75. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.48 mL 12.41 mL 24.83 mL
5 mM 0.5 mL 2.48 mL 4.97 mL
10 mM 0.25 mL 1.24 mL 2.48 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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References

References are publications that support the biological activity of the product.

Stewart et al (2004) DA D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning. J.Med.Chem. 47 2348 PMID: 15084133

Cowart et al (2004) Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a DArgic agent with a novel mode of action for the potential treatment of erectile dysfunction. J.Med.Chem. 47 3853 PMID: 15239663

Brioni et al (2004) Activation of DA D4 receptors by ABT-724 induces penile erection in rats. Proc.Natl.Acad.Sci.USA 101 6758


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Citations for ABT 724 trihydrochloride

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