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 Details
| 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 |
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| Formula: | C13H13N5O2 |
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| MW: | 271.3 |
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| CAS: | 37762-06-4 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Determined by 1H-NMR and MS. |
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| Appearance: | Pale pink to pink solid. |
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| 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. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | Ambient |
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| 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. |
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| Technical Info/Product Notes: | Note: Product is not sterile. |
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| Regulatory Status: | RUO - Research Use Only |
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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;
