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Siguazodan (CAS 115344-47-3)

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Alternate Names:
N-Cyano-N′-methyl-N′′-[4-(1,4,5,6-tetrahydro-4-methyl-6 -oxo-3-pyridazinyl)phenyl]guanidine
Application:
Siguazodan is A selective phosphodiesterase PDE III inhibitor and a potent inotropic agent
CAS Number:
115344-47-3
Purity:
≥98%
Molecular Weight:
284.3
Molecular Formula:
C14H16N6O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Siguazodan is a selective inhibitor of PDE (phosphodiesterase 3, PDE3) with an IC50 = 0.7 μM. This compound is a potent inotropic and vasodilator, with additional antiplatelet activity. Siguazodan has been shown to synergize with PDE4 inhibitors in blocking antigen-induced bronchospasm in cell models.


Siguazodan (CAS 115344-47-3) References

  1. Comparison of responses to siguazodan, rolipram, and zaprinast in the feline pulmonary vascular bed.  |  De Witt, BJ., et al. 2000. Eur J Pharmacol. 406: 233-8. PMID: 11020486
  2. Hypoxic vasoconstriction of rat main pulmonary artery: role of endogenous nitric oxide, potassium channels, and phosphodiesterase inhibition.  |  Bardou, M., et al. 2001. J Cardiovasc Pharmacol. 38: 325-34. PMID: 11483882
  3. The effects of siguazodan, a selective phosphodiesterase inhibitor, on human platelet function.  |  Murray, KJ., et al. 1990. Br J Pharmacol. 99: 612-6. PMID: 2158847
  4. Superiority of combined phosphodiesterase PDE3/PDE4 inhibition over PDE4 inhibition alone on glucocorticoid- and long-acting β2-adrenoceptor agonist-induced gene expression in human airway epithelial cells.  |  BinMahfouz, H., et al. 2015. Mol Pharmacol. 87: 64-76. PMID: 25324049
  5. In vivo pharmacological studies with SK&F 94836, a potent inotrope/vasodilator with a sustained duration of action.  |  Gristwood, RW., et al. 1988. Br J Pharmacol. 93: 893-901. PMID: 3390657
  6. Photoaffinity labelling of cyclic GMP-inhibited phosphodiesterase (PDE III) in human and rat platelets and rat tissues: effects of phosphodiesterase inhibitors.  |  Tang, KM., et al. 1994. Eur J Pharmacol. 268: 105-14. PMID: 7925608
  7. Relaxation of guinea-pig trachea by cyclic AMP phosphodiesterase inhibitors and their enhancement by sodium nitroprusside.  |  Turner, NC., et al. 1994. Br J Pharmacol. 111: 1047-52. PMID: 8032589
  8. Comparison of phosphodiesterase III, IV and dual III/IV inhibitors on bronchospasm and pulmonary eosinophil influx in guinea pigs.  |  Underwood, DC., et al. 1994. J Pharmacol Exp Ther. 270: 250-9. PMID: 8035322
  9. Rolipram, but not siguazodan or zaprinast, inhibits the excitatory noncholinergic neurotransmission in guinea-pig bronchi.  |  Qian, Y., et al. 1994. Eur Respir J. 7: 306-10. PMID: 8162984
  10. Effects of rolipram and siguazodan on the human isolated bronchus and their interaction with isoprenaline and sodium nitroprusside.  |  Qian, Y., et al. 1993. Br J Pharmacol. 109: 774-8. PMID: 8358572
  11. The effect of isoenzyme-selective PDE inhibitors on methacholine-induced contraction of guinea-pig and rat ileum.  |  Tomkinson, A. and Raeburn, D. 1996. Br J Pharmacol. 118: 2131-9. PMID: 8864552
  12. Phosphodiesterase inhibitors suppress alpha2-adrenoceptor-mediated 5-hydroxytryptamine release from tracheae of newborn rabbits.  |  Freitag, A., et al. 1998. Eur J Pharmacol. 354: 67-71. PMID: 9726632
  13. The potential roles of cytokines, IL-5 and IL-8, and plasma cortisol in the anti-inflammatory actions of phosphodiesterase inhibitors in sensitized guinea-pig airways.  |  Danahay, H., et al. 1997. Pulm Pharmacol Ther. 10: 277-85. PMID: 9778491

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Siguazodan, 5 mg

sc-201201
5 mg
$100.00

Siguazodan, 25 mg

sc-201201A
25 mg
$398.00