Specific cGMP phosphodiesterase inhibitor, selective for PDE6, 5, 11 and 9 (IC50 values are 0.15 (PDE6), 0.76 (PDE5), 12 (PDE11) and 29 μM (PDE9)). Reputed GPR35 agonist (EC50 values are 16 and 840 nM at rat and human GPR35 receptors, respectively). Important mediator for a variety of cellular processes including vasodilation.
Store at Room Temperature. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in DMSO to 25 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
Use at an assay dependent concentration.
ab76165 staining ERK1 + ERK2 (phospho T202 + Y204) in U87MG cells treated with zaprinast (ab120940), by ICC/IF. Increase of ERK1 + ERK2 (phospho T202 + Y204) expression correlates with increased concentration of zaprinast, as described in literature. The cells were incubated at 37°C for 24 hours in media containing different concentrations of ab120940 (zaprinast) in DMSO, fixed with 100% methanol for 5 minutes at -20°C and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab76165 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
This product has been referenced in:
Lugnier C Cyclic nucleotide phosphodiesterase (PDE) superfamily: a new target for the development of specific therapeutic agents. Pharmacol Ther109:366-98 (2006).
Read more (PubMed: 16102838) »
Taniguchi Y et al. Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35. FEBS Lett580:5003-8 (2006).
Read more (PubMed: 16934253) »
Soderling SH et al. Identification and characterization of a novel family of cyclic nucleotide phosphodiesterases. J Biol Chem273:15553-8 (1998).
Read more (PubMed: 9624145) »