PSB 11 hydrochloride

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Cat.No. 2012 - PSB 11 hydrochloride | C16H17N5O.HCl | CAS No. 453591-58-7
Description: Potent, selective hA3 receptor antagonist/inverse agonist
Chemical Name: (8R)-8-Ethyl-1,4,7,8-tetrahydro-4-5H-imidazo[2,1-i]purin-5-one hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective antagonist for the human adenosine A3 receptor, with low affinity for the rat A3 receptor (Ki values are 2.3 and > 10000 nM respectively). Displays > 1000-fold selectivity over human A1 and A2A receptors (Ki values are 4.1 and 3.3 μM respectively) and > 180-fold selectivity over rat A1, rat A2A and mouse A2B receptors. Acts as an inverse agonist in the [35S]GTPγS binding assay in hA3-CHO cells (IC50 = 36 nM).

Compound Libraries

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Technical Data

M. Wt 331.8
Formula C16H17N5O.HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 453591-58-7
PubChem ID 16759152
InChI Key JAUSHKIWPLHBCN-RFVHGSKJSA-N
Smiles Cl[H].CC[C@@H]1CN2C(=N1)C1=C(N=C(N1)C1=CC=CC=C1)N(C)C2=O

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 5.91 20mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 331.8. 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 3.01 mL 15.07 mL 30.14 mL
5 mM 0.6 mL 3.01 mL 6.03 mL
10 mM 0.3 mL 1.51 mL 3.01 mL
50 mM 0.06 mL 0.3 mL 0.6 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Muller et al (2002) Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A2A- and A3-adenosine receptor antagonists. J.Med.Chem. 45 3440 PMID: 12139454

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


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