PKSI-527

PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 µM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 µM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and lambda-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.Formal Name: 4-[[(2S)-2-[[[trans-4-(aminomethyl)cyclohexyl]carbonyl]amino]-1-oxo-3-phenylpropyl]amino]-benzeneacetic acid, monohydrochloride. CAS Number: 128837-71-8. Molecular Formula: C25H31N3O4 . HCl. Formula Weight: 474.0. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Water: 10 mM. SMILES: NC[C@@H]1CC[C@@H](C(N[C@@H](CC2=CC=CC=C2)C(NC3=CC=C(CC(O)=O)C=C3)=O)=O)CC1.Cl. InChi Code: InChI=1S/C25H31N3O4.ClH/c26-16-19-6-10-20(11-7-19)24(31)28-22(14-17-4-2-1-3-5-17)25(32)27-21-12-8-18(9-13-21)15-23(29)30,/h1-5,8-9,12-13,19-20,22H,6-7,10-11,14-16,26H2,(H,27,32)(H,28,31)(H,29,30),1H/t19-,20-,22-,/m0./s1. InChi Key: NAXNMKUKSBHHMP-JLBKCEDKSA-N.