Synonym
APC 366; APC 366; APC 366; APC-366 HCl; APC-366 hydrochloride
IUPAC/Chemical Name
L-Prolinamide, N2-((1-hydroxy-2-naphthalenyl)carbonyl)-L-arginyl-, monohydrochloride
InChi Key
IZLPTTJTHFFFJF-QJHJCNPRSA-N
InChi Code
InChI=1S/C22H28N6O4.ClH/c23-19(30)17-8-4-12-28(17)21(32)16(7-3-11-26-22(24)25)27-20(31)15-10-9-13-5-1-2-6-14(13)18(15)29;/h1-2,5-6,9-10,16-17,29H,3-4,7-8,11-12H2,(H2,23,30)(H,27,31)(H4,24,25,26);1H/t16-,17-;/m0./s1
SMILES Code
O=C(N)[C@H]1N(C([C@H](CCCNC(N)=N)NC(C2=CC=C3C=CC=CC3=C2O)=O)=O)CCC1.[H]Cl
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
476.96
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Matos NA, Silva JF, Damasceno KA, Cassali GD, Lemos VS, Duarte ID, Klein A. Proteinase-activated receptor 2 blockade impairs CCL11- or allergen-induced eosinophil recruitment in experimental pleurisy. Eur J Pharmacol. 2014 Oct 5;740:627-33. doi: 10.1016/j.ejphar.2014.06.018. Epub 2014 Jun 24. PubMed PMID: 24972241.
2: Lu J, Chen B, Li S, Sun Q. Tryptase inhibitor APC 366 prevents hepatic fibrosis by inhibiting collagen synthesis induced by tryptase/protease-activated receptor 2 interactions in hepatic stellate cells. Int Immunopharmacol. 2014 Jun;20(2):352-7. doi: 10.1016/j.intimp.2014.04.001. Epub 2014 Apr 13. PubMed PMID: 24735816.
3: Matos NA, Silva JF, Matsui TC, Damasceno KA, Duarte ID, Lemos VS, Cassali GD, Klein A. Mast cell tryptase induces eosinophil recruitment in the pleural cavity of mice via proteinase-activated receptor 2. Inflammation. 2013 Dec;36(6):1260-7. doi: 10.1007/s10753-013-9664-5. PubMed PMID: 23749157.
4: Duchesne E, Tremblay MH, Côté CH. Mast cell tryptase stimulates myoblast proliferation; a mechanism relying on protease-activated receptor-2 and cyclooxygenase-2. BMC Musculoskelet Disord. 2011 Oct 14;12:235. doi: 10.1186/1471-2474-12-235. PubMed PMID: 21999702; PubMed Central PMCID: PMC3207928.
5: He S, Aslam A, Gaça MD, He Y, Buckley MG, Hollenberg MD, Walls AF. 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. J Pharmacol Exp Ther. 2004 Apr;309(1):119-26. Epub 2004 Jan 13. PubMed PMID: 14722328.
