AZD 7986

AZD 7986 is a reversible and covalent inhibitor of dipeptidyl peptidase 1 (DPP-1), also known as cathepsin C (IC50 = 3.9 nM). It is selective for DPP-1 over cathepsins S, -L, -B, -K, -D, -E, -Z, -H, and -G (IC50s = >20 µM for all), as well as a panel of greater than 200 enzymes, receptors, ion channels, and transporters. AZD 7986 inhibits activation of the DPP-1 targets neutrophil elastase, proteinase 3, and cathepsin G in human bone marrow-derived CD34+ neutrophil progenitor cells (IC50s = 61.7, 208.9, and 114.8 nM, respectively). Ex vivo, AZD 7986 (0.2, 2, and 20 mg/kg) inhibits activation of neutrophil elastase and proteinase 3 in rat bone marrow lysates. AZD 7986 suppresses the formation of pulmonary and circulating neutrophil extracellular traps (NETs), increases survival, and reduces the number of lung metastases in a 4T1 murine mammary carcinoma model.Formal Name: (2S)-N-[(1S)-1-cyano-2-[4-(2,3-dihydro-3-methyl-2-oxo-5-benzoxazolyl)phenyl]ethyl]hexahydro-1,4-oxazepine-2-carboxamide. CAS Number: 1802148-05-5. Synonyms: Brensocatib, INS1007. Molecular Formula: C23H24N4O4. Formula Weight: 420.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: 2 mg/ml. SMILES: CN1C2=CC(C3=CC=C(C=C3)C[C@@H](C#N)NC([C@@H]4CNCCCO4)=O)=CC=C2OC1=O. InChi Code: InChI=1S/C23H24N4O4/c1-27-19-12-17(7-8-20(19)31-23(27)29)16-5-3-15(4-6-16)11-18(13-24)26-22(28)21-14-25-9-2-10-30-21/h3-8,12,18,21,25H,2,9-11,14H2,1H3,(H,26,28)/t18-,21-/m0/s1. InChi Key: AEXFXNFMSAAELR-RXVVDRJESA-N.