APC-366 - CAS 178925-65-0
Catalog number:
178925-65-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C22H28N6O4
Molecular Weight:
440.50
COA:
Inquire
Targets:
Others
Description:
APC-366, an amino acid derivative, has been found to be a mast cell tryptase inhibitor and was once studied against asthma by Celera Genomics Group. Ki: 7.1 μM.
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Purity:
98%
Appearance:
Powder
Synonyms:
APC 366; AC1L42OR; N-(1-Hydroxy-2-naphthoyl)-L-arginine-L-prolinamide; 158921-85-8
Solubility:
5 mg/ml in 20% ethanol / water
Storage:
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
MSDS:
Inquire
Quality Standard:
In-house standard
Quantity:
Milligram-Grams
InChIKey:
SKYWIMYOGAWOMB-IRXDYDNUSA-N
InChI:
InChI=1S/C22H28N6O4/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)/t16-,17-/m0/s1
Canonical SMILES:
C1CC(N(C1)C(=O)C(CCCN=C(N)N)NC(=O)C2=C(C3=CC=CC=C3C=C2)O)C(=O)N
1.Inhibition of mast cell tryptase by inhaled APC 366 attenuates allergen-induced late-phase airway obstruction in asthma.
Krishna MT1, Chauhan A, Little L, Sampson K, Hawksworth R, Mant T, Djukanovic R, Lee T, Holgate S. J Allergy Clin Immunol. 2001 Jun;107(6):1039-45.
BACKGROUND: APC 366, a selective inhibitor of mast cell tryptase, has been shown to inhibit antigen-induced early asthmatic response (EAR), late asthmatic response (LAR), and bronchial hyperresponsiveness (BHR) in a sheep model of allergic asthma.
2.Tryptase inhibitor APC 366 prevents hepatic fibrosis by inhibiting collagen synthesis induced by tryptase/protease-activated receptor 2 interactions in hepatic stellate cells.
Lu J1, Chen B1, Li S1, Sun Q2. Int Immunopharmacol. 2014 Jun;20(2):352-7. doi: 10.1016/j.intimp.2014.04.001. Epub 2014 Apr 13.
Protease-activated receptor (PAR) 2 is a G-protein-coupled receptor that is activated by mast cell tryptase. PAR-2 activation augments profibrotic pathways through the induction of extracellular matrix proteins. PAR-2 is widely expressed in hepatic stellate cells (HSCs), but the role of tryptase/PAR-2 interaction in liver fibrosis is unclear. We studied the development of bile duct ligation (BDL)-induced hepatic fibrosis in rats treated with mast cell tryptase inhibitor APC 366, and showed that APC 366 reduced hepatic fibrosis scores, collagen content and serum biochemical parameters. Reduced fibrosis was associated with decreased expression of PAR-2 and α-smooth muscle actin (α-SMA). Our findings demonstrate that mast cell tryptase induces PAR-2 activation to augment HSC proliferation and promote hepatic fibrosis in rats. Treatment with tryptase antagonists may be a novel therapeutic approach to prevent fibrosis in patients with chronic liver disease.
3.The tryptase inhibitor APC-366 reduces the acute airway response to allergen in pigs sensitized to Ascaris suum.
Sylvin H1, Dahlbäck M, Van Der Ploeg I, Alving K. Clin Exp Allergy. 2002 Jun;32(6):967-71.
BACKGROUND: Tryptase is a mast cell serine protease that is released during mast cell degranulation. It has been implicated as an important enzyme in the pathophysiology of asthma, but its role in this disease is not fully elucidated.
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CAS 178925-65-0 APC-366

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