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Submit ReviewZaprinast
Description: GPR35 agonist
Chemical Name: 2-(2-Propyloxyphenyl)-8-azapurin-6-one
Purity: ≥98% (HPLC)
Biological Activity for Zaprinast
Zaprinast is a 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 for Zaprinast
Zaprinast is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Zaprinast
| M. Wt | 271.28 |
| Formula | C13H13N5O2 |
| Storage | Store at RT |
| Purity | ≥98% (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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Zaprinast
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100 |
Preparing Stock Solutions for Zaprinast
The following data is based on the product molecular weight 271.28. 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 | 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 for Zaprinast
References for Zaprinast
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Zaprinast, please let us know.
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Keywords: Zaprinast, Zaprinast supplier, PDE5/6/9/11, inhibitors, inhibits, Phosphodiesterases, GPR35, 0947, Tocris Bioscience
6 Citations for Zaprinast
Citations are publications that use Tocris products. Selected citations for Zaprinast include:
Wyant et al (2022) Mitochondrial remodeling and ischemic protection by G protein–coupled receptor 35 agonists. Science 377 621 PMID: 35926043
Rojewska (2018) Kynurenic acid and zaprinast diminished CXCL17-evoked pain-related behaviour and enhanced mor. analgesia in a mouse neuropathic pain model. Pharmacol Rep 71 139 PMID: 30550994
Robichaud et al (2002) Assessing the emetic potential of PDE4 inhibitors in rats. Br J Pharmacol 135 113 PMID: 11786486
Zerani et al (2004) Ob receptor in rabbit ovary and leptin in vitro regulation of corpora lutea. J Endourol 183 279 PMID: 15531716
MacKenzie et al (2014) The antiallergic mast cell stabilizers lodox. and bufrolin as the first high and equipotent agonists of human and rat GPR35. Mol Pharmacol 85 91 PMID: 24113750
Polcari et al (2013) Effect of the phosphodiesterase-5 inhibitor zaprinast on ischemia-reperfusion injury in rats. Proc Natl Acad Sci U S A 27 338 PMID: 22974473
Do you know of a great paper that uses Zaprinast from Tocris? Please let us know.
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