PSB 10 hydrochloride

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Cat.No. 2010 - PSB 10 hydrochloride | C16H14Cl3N5O.HCl | CAS No. 591771-91-4
Description: Potent, highly selective hA3 receptor antagonist/inverse agonist
Chemical Name: 8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
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Literature

Biological Activity

Potent and highly selective antagonist for the human adenosine A3 receptor, with low affinity for the rat A3 receptor (Ki values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A1, A2A and A2B receptors (Ki values are 4.1, 3.3 and 30 μM respectively) and > 1800-fold selectivity over rat A1 and A2A receptors. Acts as an inverse agonist in the [35S]GTPγS binding assay in hA3-CHO cells (IC50 = 4 nM). Produces thermal hyperalgesia in mice in vivo.

Technical Data

M. Wt 435.14
Formula C16H14Cl3N5O.HCl
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 591771-91-4
PubChem ID 90488733
InChI Key JUPMOTHIKGWECW-DDWIOCJRSA-N
Smiles CC[C@H](C3)N=C1N3C(N(C)C2=C1NC(C4=C(Cl)C(Cl)=CC(Cl)=C4)=N2)=O.Cl

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

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.88 25
ethanol 4.35 10

Preparing Stock Solutions

The following data is based on the product molecular weight 435.14. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.3 mL 11.49 mL 22.98 mL
5 mM 0.46 mL 2.3 mL 4.6 mL
10 mM 0.23 mL 1.15 mL 2.3 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

Muller (2003) Medicinal chemistry of adenosine A3 receptor ligands. Curr.Top.Med.Chem. 3 445 PMID: 12570761

Ozola et al (2003) 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at human A3 adenosine receptors. Bioorg.Med.Chem. 11 347 PMID: 12517430

Abo-Salem et al (2004) Antinociceptive effects of novel A2B adenosine receptor antagonists. J.Pharmacol.Exp.Ther. 308 358 PMID: 14563788


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