A mast cell tryptase inhibitor
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APC 366 (trifluoroacetate salt)

Item No. 25990

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-[(1-hydroxy-2-naphthalenyl)carbonyl]-L-arginyl-L-prolinamide, trifluoroacetate salt
Molecular Formula
C22H28N6O4 • XCF3COOH
Formula Weight
440.5
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Ethanol:Water: 5 mg/ml (in 20% EtOH)
SMILES
OC1=C(C(N[C@@H](CCCNC(N)=N)C(N2[C@H](C(N)=O)CCC2)=O)=O)C=CC3=CC=CC=C31.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C22H28N6O4.C2HF3O2/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;3-2(4,5)1(6)7/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);(H,6,7)/t16-,17-;/m0./s1
InChi Key
FFLIQFBAKJNSSS-QJHJCNPRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    Cayman Chemical
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    Product Description

    APC 366 is a mast cell tryptase inhibitor (Ki = 7.1 μM for human recombinant enzyme).1 It reduces maximum contractile response to histamine in isolated bronchial tissue from ovalbumin-sensitized guinea pigs when used at a concentration of 1 μM. Aerosolized APC 366 (5 mg in 1 ml of water) reduces airway resistance and increases dynamic lung compliance in A. suum antigen-challenged pigs.2 It also reduces collagen content and expression of protease-activated receptor 2 (PAR-2) and α-smooth muscle actin (α-SMA) in rat liver in a model of bile duct ligation-induced liver fibrosis.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Barrios, V.E., Middleton, S.C., Kashem, M.A., et al. Tryptase mediates hyperresponsiveness in isolated guinea pig bronchi. Life Sci. 63(26), 2295-2303 (1998).

    2. Sylvin, H., Dahlbäck, M., Van Der Ploeg, I., et al. The tryptase inhibitor APC-366 reduces the acute airway response to allergen in pigs sensitized to Ascaris suum. Clin. Exp. Allergy 32(6), 967-971 (2002).

    3. Lu, J., Chen, B., Li, S., et al. 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. 20(2), 352-357 (2014).