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Zaprinast

PDE inhibitor
 
BML-PD190-0100 100 mg 212.00 USD
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Replaces Prod. #: ALX-430-020

Selective inhibitor of cGMP-specific phosphodiesterase (PDE5: IC50=0.2-0.8µM, PDE1: IC50=2.6µM, PDE2: IC50>10µM, PDE3: IC50>10µM, PDE4: IC50>10µM). Increases cGMP levels in SHR plasma. Reverses nitroglycerin tolerance in vitro .

Product Specification

Alternative Name:M&B 22,948, 1,4-Dihydro-5-[2-propoxyphenyl]-7H-1,2,3-triazolo[4,5-d]pyrimidine-7-one, 2-(2-Propoxyphenyl)-8-azahypoxanthine
 
Formula:C13H13N5O2
 
MW:271.3
 
CAS:37762-06-4
 
Purity:≥98% (HPLC)
 
Identity:Determined by 1H-NMR and MS.
 
Appearance:Pale pink to pink solid.
 
Solubility:Soluble in 1M sodium hydroxide, 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin (0.11mg/ml), DMSO (25mg/ml) or 100% ethanol (5 mg/ml); insoluble in water.
 
Shipping:Ambient
 
Long Term Storage:Ambient
 
Use/Stability:Stable for up to 5 years after receipt when stored at +20°C. Stock solutions are stable for up to 6 months at -20°C.
 
Technical Info/Product Notes:Note: Product is not sterile.
 
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Product Literature References

Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35: Y. Taniguchi, et al.; FEBS Lett. 580, 5003 (2006), Abstract;
Phosphodiesterase 5 inhibitor, zaprinast, selectively increases cerebral blood flow in the ischemic penumbra in the rat brain: F. Gao, et al.; Neurol. Res. 27, 638 (2005), Abstract;
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 1: 5,6,11,11a-tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione analogues: A. Daugan, et al.; J. Med. Chem. 46, 4525 (2003), Abstract;
The PDE inhibitor zaprinast enhances NO-mediated protection against vascular leakage in reperfused lungs: H. Schutte, et al.; Am. J. Physiol. Lung Cell Mol. Physiol. 279, L496 (2000), Abstract; Full Text
The nitric oxide--cyclic GMP pathway and synaptic depression in rat hippocampal slices: C.L. Boulton, et al.; Eur. J. Neurosci. 6, 1528 (1994), Abstract;
Reversal of nitroglycerin tolerance in vitro by the cGMP- phosphodiesterase inhibitor zaprinast: E.D. Pagani, et al.; Eur. J. Pharmacol. 243, 141 (1993), Abstract;
Zaprinast increases cyclic GMP levels in plasma and in aortic tissue of rats: R.L. Dundore, et al.; Eur. J. Pharmacol. 249, 293 (1993), Abstract;
Cyclic nucleotide phosphodiesterases from frog atrial fibers: isolation and drug sensitivities: C. Lugnier, et al.; Am. J. Physiol. 262, H654 (1992), Abstract;
The catalytic subunit of protein kinase A triggers activation of the type V cyclic GMP-specific phosphodiesterase from guinea-pig lung: F. Burns, et al.; Biochem. J. 283, 487 (1992), Abstract;
Primary sequence of cyclic nucleotide phosphodiesterase isozymes and the design of selective inhibitors: J.A. Beavo & D.H. Reifsnyder; TIPS 11, 150 (1990), Abstract;
Inhibition and stimulation of photoreceptor phosphodiesterases by dipyridamole and M&B 22,948: P.G. Gillespie and J.A. Beavo; Mol. Pharmacol. 36, 773 (1989), Abstract;

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