APC 366

An elective, selective inhibitor of the mast cell tryptase, which inhibits tryptase-induced histamine release from human tonsil and lung cells. It can reduce airway inflammation and block postchallenge airway hyperresponsiveness in vivo.

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CAT#	R0892
CAS	158921-85-8
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. >> Read More
Synonyms/Alias	N-(1-Hydroxy-2-naphthoyl)-L-arginyl-L-prolinamide
M.F/Formula	C22H28N6O4
M.W/Mr.	440.5
Sequence	N-(1-Hydroxy-2-naphthoyl)-L-arginyl-L-prolinamide
Labeling Target	Tryptase
Appearance	White lyophilised solid
Purity	>98%
Activity	Inhibitor

CAT#	Product Name	M.W	Molecular Formula	Inquiry
R0937	NFAT inhibitor, Cell Permeable	3573.15	C147H259N67O36S	Inquiry
R0951	Ac-Ala-Asn-Trp-AMC (Ac-ANW-AMC)	588.6	C30H32N6O7	Inquiry
R1025	Z-Leu-Leu-Glu-AMC	664.76	C₃₅H₄₄N₄O₉	Inquiry
R1026	Z-Leu-Arg-Gly-Gly-AMC	692.77	C₃₄H₄₄N₈O₈	Inquiry
R1032	Chlorotoxin	599.64	C29H37N5O9S1	Inquiry

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Source#	Synthetic
Storage	-20°C
Long-term Storage Conditions	-20 °C
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
InChI Key	SKYWIMYOGAWOMB-IRXDYDNUSA-N
Isomeric SMILES	C1C[C@H](N(C1)C(=O)[C@H](CCCN=C(N)N)NC(=O)C2=C(C3=CC=CC=C3C=C2)O)C(=O)N
References	In sheep naturally sensitized to Ascaris suum , the novel selective inhibitor of tryptase APC 366 [N-(1-hydroxy-2-naphthoyl)-L-arginyl-L-prolinamide] attenuates the EAR, the LAR, acquired BHR, and the accompanying influx of inflammatory leukocytes on aerosol challenge with an antigenic extract. It has been shown that APC 366 inactivates tryptase in a time-dependent and irreversible manner involving slow isomerization of the hydroxynaphthyl group of APC 366 followed by nucleophilic attack of a tryptase amino acid side chain to result in the formation of a nonhydrolyzable covalent adduct between inhibitor and enzyme. Inhibition of mast cell tryptase by inhaled APC 366 attenuates allergen-induced late-phase airway obstruction in asthma