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Submit ReviewZaprinast
说明： GPR35 agonist
化学名： 2-(2-Propyloxyphenyl)-8-azapurin-6-one
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for Zaprinast
Zaprinast is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Zaprinast
| 分子量 | 271.28 |
| 公式 | C13H13N5O2 |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Zaprinast
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 100 |
制备储备液 for Zaprinast
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Zaprinast
参考文献 for Zaprinast
参考文献是支持产品生物活性的出版物。
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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关键词: Zaprinast, Zaprinast supplier, PDE5/6/9/11, inhibitors, inhibits, Phosphodiesterases, GPR35, 0947, Tocris Bioscience
6 篇 Zaprinast 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Zaprinast 的部分引用包括：
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
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