684500
Zaprinast - CAS 37762-06-4 - Calbiochem
A cell-permeable, selective inhibitor of cGMP-specific phosphodiesterase (PDE V; IC50 = 450 nM).
Synonym(s):
Zaprinast - CAS 37762-06-4 - Calbiochem, 1,4-Dihydro-5-(2-propoxyphenyl)-7H-1,2,3-triazolo[4,5-d]pyrimidine-7-one, M&B22948
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About This Item
Empirical Formula (Hill Notation):
C13H13N5O2
CAS Number:
Molecular Weight:
271.27
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
solid
potency
450 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
tan to pink
solubility
DMSO: 25 mg/mL, ethanol: 5 mg/mL
shipped in
ambient
storage temp.
10-30°C
InChI
1S/C13H13N5O2/c1-2-7-20-9-6-4-3-5-8(9)11-14-12-10(13(19)15-11)16-18-17-12/h3-6H,2,7H2,1H3,(H2,14,15,16,17,18,19)
InChI key
REZGGXNDEMKIQB-UHFFFAOYSA-N
General description
A cell-permeable, selective inhibitor of cGMP-specific phosphodiesterase (PDE V; IC50 = 450 nM). Inhibits PDE IX at higher concentration (IC50 = 35 µM). Also known to increase cGMP levels in spontaneously hypertensive rat (SHR) plasma and reverse nitroglycerin tolerance in vitro. Enhances the vasodilatory effects of nitric oxide.
Selective inhibitor of cGMP-specific phosphodiesterase (PDE V, IC50 = 450 nM). Also known to increase cGMP levels in SHR plasma and reverse nitroglycerin tolerance in vitro. Enhances the vasodilatory effects of nitric oxide.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
cGMP-specific phosphodiesterase
cGMP-specific phosphodiesterase
Product does not compete with ATP.
Reversible: no
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.
From Catalog:
Desc. Field- added "cell-permeable"
From Catalog:
Desc. Field- added "cell-permeable"
Other Notes
Fisher, D.A., et al. 1998. J. Biol. Chem. 273, 15559.
Tsusu, K.G., et al. 1995. Am. J. Respir. Crit. Care Med.152, 1605.
Dundore, R.L., et al. 1993. Eur. J. Pharmacol.249, 293.
Pagani, E.D., et al. 1993. Eur. J. Pharmacol.243, 141.
Burns, F., et al. 1992. Biochem. J.283, 487.
Lugnier, C., et al. 1992. Am. J. Physiol.262, H654.
Tsusu, K.G., et al. 1995. Am. J. Respir. Crit. Care Med.152, 1605.
Dundore, R.L., et al. 1993. Eur. J. Pharmacol.249, 293.
Pagani, E.D., et al. 1993. Eur. J. Pharmacol.243, 141.
Burns, F., et al. 1992. Biochem. J.283, 487.
Lugnier, C., et al. 1992. Am. J. Physiol.262, H654.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
Storage Class
10-13 - German Storage Class 10 to 13
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Alice L Herneisen et al.
eLife, 13 (2024-08-13)
Apicomplexan parasites balance proliferation, persistence, and spread in their metazoan hosts. AGC kinases, such as PKG, PKA, and the PDK1 ortholog SPARK, integrate environmental signals to toggle parasites between replicative and motile life stages. Recent studies have cataloged pathways downstream
H Ji
Methods in molecular medicine, 51, 363-377 (2001-01-01)
Angiotensin type-1 receptors (AT(1) receptors) mediate various physiological actions of angiotensin (Ang II) via multiple-signal transduction pathways (1). In addition to the phospholipase C pathway and dihydropyridine-sensitive voltage-dependent calcium channels, AT(1) receptors can couple to inhibition of adenylate cyclase via
Alex W Chan et al.
eLife, 12 (2023-11-07)
Apicomplexan parasites use Ca2+-regulated exocytosis to secrete essential virulence factors from specialized organelles called micronemes. Ca2+-dependent protein kinases (CDPKs) are required for microneme exocytosis; however, the molecular events that regulate trafficking and fusion of micronemes with the plasma membrane remain