APC 366

APC 366 is a selective and competitive inhibitor of tryptase [1, 2, 3]. After about 4 h of incubation with human tryptase, APC 366 showed an inhibitory potential with a Ki value of 530 nM and an IC50 value of 1400 ± 240 nM . Tryptase is a mast cell serine protease. It had been implicated in the allergic asthma pathophysiology . It seemed that actions of tryptase were dependent on an intact catalytic site. APC 366 inhibited DNA synthesis and the proliferation of the smooth muscle cell (SMC) induced by tryptase. In this study, thymidine incorporation was reduced by APC 366 by 79%. Heating to inactivate enzymatic activity also abolished the ability of tryptase to stimulate SMC proliferation and DNA synthesis . In urine in the control pigs, the concentration of histamine was immediately elevated after allergen challenge. But treatment with APC 366 markedly decreased this release . In vivo in a sheep model, administration with APC 366 decreased allergen-induced early and late-phase bronchoconstriction and hyperresponsiveness . In allergic sheep, APC 366 was administered by aerosol in all experiments. In vehicle control trials, antigen challenge caused peak early and late increases in specific lung resistance with values of 259 ± 30% and 183 ± 27% over baseline, respectively. 0.5 h before, 4 h after and 24 h after antigen challenge, treatment with APC 366 at 9 mg/3 ml H2O slightly decreased the peak early response (194 ± 41%) and significantly inhibited the late response (38 ± 6%, p < 0.05) .

Product information

CAS Number: 158921-85-8

Molecular Weight: 440.50

Formula: C22H28N6O4

Chemical Name: (2S)-1-[(2S)-5-carbamimidamido-2-[(1-hydroxynaphthalen-2-yl)formamido]pentanoyl]pyrrolidine-2-carboxamide

Smiles: NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)C1C=CC2=CC=CC=C2C=1O

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.