Cathepsin G Inhibitor I

Cathepsin G inhibitor I is an inhibitor of cathepsin G (IC50 = 53 nM). It is selective for cathepsin G over various serine proteases, including thrombin, Factor Xa, Factor IXa, plasmin, trypsin, and leukocyte proteinase 3 (PR3, IC50s = >100 µM for all), but also weakly inhibits chymotrypsin. It inhibits cathepsin G-induced activation of IL-36 in neutrophil degranulates when used at a concentration of 10 µM. Cathepsin G inhibitor I (10 µM) reduces CD4+ T cell-induced secretion of IFN-gamma and IL-17 in B cells incubated with tetanus toxin C-fragments (TTC) and also reduces TTC presentation in B cells. It decreases the size of neuromyelitis optica lesions and reduces the number of perivascular neutrophils, indicating decreased neutrophil brain entry, when used in combination with the neutrophil elastase inhibitor sivelestat (Cay-17779) in a mouse model of IgG-induced brain injury when administered intracerebrally at a dose of 5 µg/animal.Formal Name: P-[2-[3-[[(1-benzoyl-4-piperidinyl)methylamino]carbonyl]-2-naphthalenyl]-1-(1-naphthalenyl)-2-oxoethyl]-phosphonic acid. CAS Number: 429676-93-7. Molecular Formula: C36H33N2O6P. Formula Weight: 620.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 224, 248 nm. SMILES: O=C(N(C1CCN(C(C2=CC=CC=C2)=O)CC1)C)C3=CC4=CC=CC=C4C=C3C(C(C5=CC=CC6=C5C=CC=C6)P(O)(O)=O)=O. InChi Code: InChI=1S/C36H33N2O6P/c1-37(28-18-20-38(21-19-28)35(40)25-11-3-2-4-12-25)36(41)32-23-27-14-6-5-13-26(27)22-31(32)33(39)34(45(42,43)44)30-17-9-15-24-10-7-8-16-29(24)30/h2-17,22-23,28,34H,18-21H2,1H3,(H2,42,43,44). InChi Key: GNOZQRKYZJSIPZ-UHFFFAOYSA-N.