Date published: 2025-12-5

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Tolafentrine (CAS 139308-65-9)

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Alternate Names:
rel-(−)-N-[4-[(4aR,10bS)-1,2,3,4,4a,10b-Hexahydro-8,9-dimethoxy-2-methylbenzo[c][1,6]naphthyridin-6-yl]phenyl]-4-methylbenzenesulfonamide
Application:
Tolafentrine is A dual-selective phosphodiesterase 3/4 inhibitor.
CAS Number:
139308-65-9
Molecular Weight:
505.63
Molecular Formula:
C28H31N3O4S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Tolafentrine is a pharmacological compound characterized by its dual-selective inhibition of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4). The research on Tolafentrine and similar dual-selective PDE inhibitors is for advancing our understanding of pulmonary hypertension′s complex pathophysiology. It highlights the importance of targeted therapies that can simultaneously address multiple pathways involved in the adverse biological process.


Tolafentrine (CAS 139308-65-9) References

  1. Low-dose systemic phosphodiesterase inhibitors amplify the pulmonary vasodilatory response to inhaled prostacyclin in experimental pulmonary hypertension.  |  Schermuly, RT., et al. 1999. Am J Respir Crit Care Med. 160: 1500-6. PMID: 10556112
  2. Subthreshold doses of specific phosphodiesterase type 3 and 4 inhibitors enhance the pulmonary vasodilatory response to nebulized prostacyclin with improvement in gas exchange.  |  Schermuly, RT., et al. 2000. J Pharmacol Exp Ther. 292: 512-20. PMID: 10640287
  3. Complete reversal of fatal pulmonary hypertension in rats by a serine elastase inhibitor.  |  Cowan, KN., et al. 2000. Nat Med. 6: 698-702. PMID: 10835689
  4. Monocyte membrane type 1-matrix metalloproteinase. Prostaglandin-dependent regulation and role in metalloproteinase-2 activation.  |  Shankavaram, UT., et al. 2001. J Biol Chem. 276: 19027-32. PMID: 11259424
  5. Coaerosolization of phosphodiesterase inhibitors markedly enhances the pulmonary vasodilatory response to inhaled iloprost in experimental pulmonary hypertension. Maintenance of lung selectivity.  |  Schermuly, RT., et al. 2001. Am J Respir Crit Care Med. 164: 1694-700. PMID: 11719312
  6. Cyclic AMP increases endogenous granulocyte colony-stimulating factor formation in monocytes and THP-1 macrophages despite attenuated TNF-alpha formation.  |  Hareng, L., et al. 2003. Eur J Immunol. 33: 2287-96. PMID: 12884304
  7. Antiremodeling effects of iloprost and the dual-selective phosphodiesterase 3/4 inhibitor tolafentrine in chronic experimental pulmonary hypertension.  |  Schermuly, RT., et al. 2004. Circ Res. 94: 1101-8. PMID: 15031263
  8. Inhaled tolafentrine reverses pulmonary vascular remodeling via inhibition of smooth muscle cell migration.  |  Pullamsetti, S., et al. 2005. Respir Res. 6: 128. PMID: 16262900
  9. cAMP phosphodiesterase inhibitors increases nitric oxide production by modulating dimethylarginine dimethylaminohydrolases.  |  Pullamsetti, SS., et al. 2011. Circulation. 123: 1194-204. PMID: 21382892
  10. Activation and pulmonary toxicity of pyrrolizidine alkaloids.  |  Huxtable, RJ. 1990. Pharmacol Ther. 47: 371-89. PMID: 2290854
  11. Differential effects of non-selective and selective phosphodiesterase inhibitors on human eosinophil functions.  |  Hatzelmann, A., et al. 1995. Br J Pharmacol. 114: 821-31. PMID: 7539697
  12. Cyclic AMP-regulated synthesis of the tissue inhibitors of metalloproteinases suppresses the invasive potential of the human fibrosarcoma cell line HT1080.  |  Tanaka, K., et al. 1995. Cancer Res. 55: 2927-35. PMID: 7796421
  13. Phosphodiesterase inhibition improves agonist-induced relaxation of hypertensive pulmonary arteries.  |  Wagner, RS., et al. 1997. J Pharmacol Exp Ther. 282: 1650-7. PMID: 9316883

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Tolafentrine, 5 mg

sc-208443
5 mg
$439.00