10010421  Zaprinast

2-(o-Propoxyphenyl)-8-azapurin-6-one; M&B 22,948 (CAS 37762-06-4)

Click image to enlarge


Chemical structure definitions are available for many Cayman products. See Chemical Structure Database for details.

The cyclic nucleotide second messenger guanosine 3’5’-cyclic monophosphate (cGMP) is an important mediator of signal transduction and hence a wide range of cellular processes. It can be generated by soluble guanylyl cyclase in response to binding of nitric oxide and degraded via members of the phosphodiesterase (PDE) protein family. Zaprinast, the compound from which sildenafil (Viagra™) was developed, is a cGMP-specific phosphodiesterase inhibitor. It moderately inhibits PDE5 and PDE6 with IC50 values of 0.5-0.76 and 0.15 µM, respectively, and weakly inhibits PDE9, PDE10, and PDE11 with IC50 values of 35, 22, and 11-33 µM, respectively.1,2 Zaprinast therefore enhances the vasodilatory effects of nitric oxide in a range of vascular tissues by prolonging the cGMP-mediated activation of cGMP-dependent protein kinase.2 Zaprinast also activates both the rat and human G protein-coupled receptor, GPR35 with EC50 values of 16 nM and 0.84 µM, respectively.3
1  Nakamizo, T., Kawamata, J., Yoshida, K., et al. Phosphodiesterase inhibitors are neuroprotective to cultured spinal motor neurons. J Neurosci Res 71 485-495 (2003).
2  Gibson, A. Phosphodiesterase 5 inhibitors and nitrergic transmission-from zaprinast to sildenafil. Eur J Pharmacol 411 1-10 (2001).
3  Taniguchi, Y., Tonai-Kachi, H., Shinjo, K. Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35. FEBS Lett 580 5003-5008 (2006).


Purchase 10010421 Zaprinast

Pricing is for North America only. Other customers should contact a distributor in their region.

This product is also available to buy in bulk quantities. Please contact our Sales Department for a quote or to purchase.

Cayman strives to be a reliable biochemical reagent vendor by providing the best possible products and services. To ask for assistance with one of our products please contact our Technical Help staff.

Warning This product is not for human or veterinary use.

Pricing updated 2010-02-09.
Prices are subject to change without notice.

Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.

  email: password: hide x LOGIN | REGISTER
Cayman Chemical
Topical Catalogs
Packed with articles, the latest products, and much more.

New
Eicosanoid


Allergy, Asthma, & Inflammation

Cancer

More...
Helping to make your research possible by providing quality biochemicals and assays for research in and much more.
toll free 800.364.9897
direct dial 734.971.3335
1180 East Ellsworth Road
Ann Arbor, Michigan 48108
USA