Zaprinast

http://dbpedia.org/resource/Zaprinast an entity of type: Thing

Zaprinast was an unsuccessful clinical drug candidate that was a precursor to the chemically related PDE5 inhibitors, such as sildenafil (Viagra), which successfully reached the market. It is a phosphodiesterase inhibitor, selective for the subtypes PDE5, PDE6, PDE9 and PDE11. IC50 values are 0.76, 0.15, 29.0, and 12.0 μM, respectively. Zaprinast inhibits the growth of asexual blood-stage malaria parasites (P. falciparum) in vitro with an ED50 value of 35 μM, and inhibits PfPDE1, a P. falciparum cGMP-specific phosphodiesterase, with an IC50 value of 3.8 μM. rdf:langString
rdf:langString Zaprinast
xsd:integer 30440819
xsd:integer 1048447841
rdf:langString Zaprinast.svg
xsd:integer 150
xsd:integer 5
rdf:langString M&B 22,948
rdf:langString changed
xsd:integer 470635612
rdf:langString Zaprinast was an unsuccessful clinical drug candidate that was a precursor to the chemically related PDE5 inhibitors, such as sildenafil (Viagra), which successfully reached the market. It is a phosphodiesterase inhibitor, selective for the subtypes PDE5, PDE6, PDE9 and PDE11. IC50 values are 0.76, 0.15, 29.0, and 12.0 μM, respectively. Zaprinast inhibits the growth of asexual blood-stage malaria parasites (P. falciparum) in vitro with an ED50 value of 35 μM, and inhibits PfPDE1, a P. falciparum cGMP-specific phosphodiesterase, with an IC50 value of 3.8 μM. Zaprinast has also been shown to activate the orphan G-protein coupled receptor known as GPR35, both in rats and humans, and to inhibit the mitochondrial pyruvate carrier.
xsd:nonNegativeInteger 5486
rdf:langString M&B 22,948
rdf:langString 5-(2-Propoxyphenyl)-1H-[1,2,3]triazolo[4,5-d]pyrimidin-7(4H)-one

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