Date published: 2025-12-18

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APC 366 (CAS 158921-85-8)

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Alternate Names:
N-(1-Hydroxy-2-naphthoyl)-L-arginyl-L-prolinamide
Application:
APC 366 is a elective inhibitor of the mast cell tryptase
CAS Number:
158921-85-8
Purity:
≥96%
Molecular Weight:
440.49
Molecular Formula:
C22H28N6O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.

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Selective inhibitor of the mast cell tryptase (Ki = 7.1 µM) that inhibits tryptase-induced histamine release from human tonsil and lung cells. APC 366 has been observed to impede the activity of cyclooxygenase-2 (COX-2), an enzyme in the synthesis of pro-inflammatory cytokines. Additionally, the compound has demonstrated the ability to activate the anti-inflammatory nuclear factor-kappa B (NF-κB) signaling pathway.


APC 366 (CAS 158921-85-8) References

  1. Inhibitors of tryptase for the treatment of mast cell-mediated diseases.  |  Rice, KD., et al. 1998. Curr Pharm Des. 4: 381-96. PMID: 10197050
  2. The tryptase inhibitor APC-366 reduces the acute airway response to allergen in pigs sensitized to Ascaris suum.  |  Sylvin, H., et al. 2002. Clin Exp Allergy. 32: 967-71. PMID: 12047446
  3. Inhibitors of tryptase as mast cell-stabilizing agents in the human airways: effects of tryptase and other agonists of proteinase-activated receptor 2 on histamine release.  |  He, S., et al. 2004. J Pharmacol Exp Ther. 309: 119-26. PMID: 14722328
  4. Tryptase inhibitors: a novel class of anti-inflammatory drugs.  |  Numerof, RP., et al. 1997. Expert Opin Investig Drugs. 6: 811-7. PMID: 15989643
  5. Mast cell tryptase stimulates myoblast proliferation; a mechanism relying on protease-activated receptor-2 and cyclooxygenase-2.  |  Duchesne, E., et al. 2011. BMC Musculoskelet Disord. 12: 235. PMID: 21999702
  6. Mast cell tryptase induces eosinophil recruitment in the pleural cavity of mice via proteinase-activated receptor 2.  |  Matos, NA., et al. 2013. Inflammation. 36: 1260-7. PMID: 23749157
  7. Tryptase inhibitor APC 366 prevents hepatic fibrosis by inhibiting collagen synthesis induced by tryptase/protease-activated receptor 2 interactions in hepatic stellate cells.  |  Lu, J., et al. 2014. Int Immunopharmacol. 20: 352-7. PMID: 24735816
  8. Proteinase-activated receptor 2 blockade impairs CCL11- or allergen-induced eosinophil recruitment in experimental pleurisy.  |  Matos, NA., et al. 2014. Eur J Pharmacol. 740: 627-33. PMID: 24972241
  9. A role for mast cells in geographic atrophy.  |  Ogura, S., et al. 2020. FASEB J. 34: 10117-10131. PMID: 32525594
  10. Tryptase inhibitors block allergen-induced airway and inflammatory responses in allergic sheep.  |  Clark, JM., et al. 1995. Am J Respir Crit Care Med. 152: 2076-83. PMID: 8520778
  11. Guinea pig lung tryptase. Localisation to mast cells and characterisation of the partially purified enzyme.  |  McEuen, AR., et al. 1996. Biochem Pharmacol. 52: 331-40. PMID: 8694858
  12. Inhaled tryptase causes bronchoconstriction in sheep via histamine release.  |  Molinari, JF., et al. 1996. Am J Respir Crit Care Med. 154: 649-53. PMID: 8810600
  13. Role of tryptase in immediate cutaneous responses in allergic sheep.  |  Molinari, JF., et al. 1995. J Appl Physiol (1985). 79: 1966-70. PMID: 8847261
  14. A role for tryptase in the activation of human mast cells: modulation of histamine release by tryptase and inhibitors of tryptase.  |  He, S., et al. 1998. J Pharmacol Exp Ther. 286: 289-97. PMID: 9655871
  15. Tryptase mediates hyperresponsiveness in isolated guinea pig bronchi.  |  Barrios, VE., et al. 1998. Life Sci. 63: 2295-303. PMID: 9877219

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

APC 366, 5 mg

sc-203516
5 mg
$239.00
US: Only available in the US