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ZAPRINAST

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ZAPRINAST Basic information

Product Name:
ZAPRINAST
Synonyms:
  • 1,4-DIHYDRO-5-[2-PROPOXYPHENYL]-7H-1,2,3-TRIAZOLO[4,5-D]PYRIMIDINE-7-ONE
  • 2-(o-Propoxyphenyl)-8-azapurin-6-one
  • 5-(2-propoxyphenyl)-2,3-dihydro-[1,2,3]triazolo[4,5-d]pyrimidin-7-one
  • 5-(2-propoxyphenyl)-2,3-dihydrotriazolo[4,5-d]pyrimidin-7-one
  • 3,6-dihydro-5-(2-propoxyphenyl)-
  • Zaprinast (M&B 22948)
  • Zaprinast - CAS 37762-06-4 - Calbiochem
  • 5-(2-Propoxyphenyl)-1H-[1,2,3]triazolo[4,5-d]pyrimidin-7(4H)-one
CAS:
37762-06-4
MF:
C13H13N5O2
MW:
271.27
EINECS:
253-655-1
Product Categories:
  • All Inhibitors
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Cyclic Nucleotide related
Mol File:
37762-06-4.mol
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ZAPRINAST Chemical Properties

Melting point:
237-238°C dec.
Density 
1.48±0.1 g/cm3(Predicted)
RTECS 
XZ6157358
storage temp. 
Store at RT
solubility 
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.11 mg/mL
pka
6.92±0.20(Predicted)
form 
solid
color 
white
CAS DataBase Reference
37762-06-4
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Safety Information

Hazard Codes 
Xi
Risk Statements 
36/37/38
Safety Statements 
26-36
WGK Germany 
3

MSDS

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ZAPRINAST Usage And Synthesis

Description

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. 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. Zaprinast also activates both the rat and human G protein-coupled receptor, GPR35 with EC50 values of 16 nM and 0.84 μM, respectively.

Chemical Properties

Zaprinast is Yellow-Orange Crystalline Powder

Uses

cGMP phosphodiesterase inhibitor

Uses

Zaprinast is  a  selective inhibitor of cyclic-GMP phosphodiesterase (PDE V, calmodulin insensitive). Since cGMP mediates the vasorelaxant action of nitric oxide, as well as the natriuretic and diuretic effect of at rial natriuretic factor (ANF) through the activation of PKG (cGMP dependent protein kinase), such inhibitors may display vasodilating, relaxant, and diuretic effects. These compounds may prove useful in treating hypertension and congestive heart failure.

Uses

Zaprinast has been used to determine its inhibitory effect on the meiosis of oocytes by germinal vesicle breakdown (GVBD) assay and to test the inhibitory effect of it on the retinal cells by immunohistochemistry.

Biological Activity

Phosphodiesterase inhibitor, selective for PDE6, 5, 11 and 9 (IC 50 values are 0.15, 0.76, 12.0 and 29.0 μ M respectively).

Biochem/physiol Actions

Zaprinast insubstantially inhibits phosphodiesterase 10 and 11 (PDE10 and PDE11). It also exhibits vasodilating effects.

ZAPRINASTSupplier

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