Biological Activity
Selective adenosine A1 receptor antagonist; displays 890-fold selectivity for rat A1 receptors over A2A receptors (Ki values are 0.19 and 170 nM respectively). Displays no effect on recombinant rat A3 receptors expressed on CHO cells at concentrations up to 10 μM. Exhibits diuretic and renal protective effects in rats.
Compound Libraries
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Technical Data
| M. Wt | 356.46 |
| Formula | C20H28N4O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 136199-02-5 |
| PubChem ID | 64627 |
| InChI Key | PJBFVWGQFLYWCB-UHFFFAOYSA-N |
| Smiles | O=C1C2=C(NC(C34CC(CC4C5)CC5C3)=N2)N(CCC)C(N1CCC)=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 | 17.82 | 50 | |
| ethanol | 8.91 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 356.46. 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 | 2.81 mL | 14.03 mL | 28.05 mL |
| 5 mM | 0.56 mL | 2.81 mL | 5.61 mL |
| 10 mM | 0.28 mL | 1.4 mL | 2.81 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Shimada et al (1992) 8-polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors. J.Med.Chem. 35 924 PMID: 1548682
Nonaka et al (1996) KW-3902, a selective high affinity antagonist for adenosine A1 receptors. Br.J.Pharmacol. 117 1645 PMID: 8732272
Nishiyama et al (1999) Adenosine A1 receptor antagonist KW-3902 prevents hypoxia-induced renal vasoconstriction. J.Pharmacol.Exp.Ther. 291 988 PMID: 10565815
Keywords: KW 3902, supplier, adenosine, a1, antagonists, selective, KW3902, Rolofylline, Adenosine, A1, Receptors, Adenosine, A1, Receptors, Tocris Bioscience
