Biological Activity
Phosphodiesterase inhibitor, selective for PDE6, 5, 11 and 9 (IC50 values are 0.15, 0.76, 12.0 and 29.0 μM respectively). Putative GPR35 agonist.
Compound Libraries
Zaprinast is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 271.28 |
| Formula | C13H13N5O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 37762-06-4 |
| PubChem ID | 5722 |
| InChI Key | REZGGXNDEMKIQB-UHFFFAOYSA-N |
| Smiles | CCCOC1=C(C=CC=C1)C1=NC2=C(NN=N2)C(=O)N1 |
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
| Solubility | Soluble to 100 mM in DMSO |
Preparing Stock Solutions
The following data is based on the product molecular weight 271.28. 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 | 3.69 mL | 18.43 mL | 36.86 mL |
| 5 mM | 0.74 mL | 3.69 mL | 7.37 mL |
| 10 mM | 0.37 mL | 1.84 mL | 3.69 mL |
| 50 mM | 0.07 mL | 0.37 mL | 0.74 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Lugnier (2006) Cyclic nucleotide phosphodiesterase (PDE) superfamily: a new target for the development of specific therapeutic agents. Pharmacol.Ther. 109 366 PMID: 16102838
Soderling et al (1998) Identification and characterization of a novel family of cyclic nucleotide phosphodiesterases. J.Biol.Chem. 273 15553 PMID: 9624145
Taniguchi et al (2006) Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35. FEBS Lett. 580 5003 PMID: 16934253
Christensen and Torphy (1994) Isozyme-selective phosphodiesterase inhibitors as antiasthmatic agents. Annu.Rep.Med.Chem. 29 185 PMID:
Keywords: Zaprinast, supplier, PDE5/6/9/11, inhibitors, inhibits, Phosphodiesterases, Phosphodiesterases, GPR35, GPR35, Tocris Bioscience
