AZD7986, inhibitor

AZD7986

Cat. Num. AAA5764296

• Purity: 98.00%
• Synonyms: AZD7986; INS 1007; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (237.83mM); Water: Insoluble; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C23H22N4O4
• SMILES: O=C([C@]1OCCCNC1)N[C@](C#N)CC2=CC=C(C3=CC=C(OC(N4C)=O)C4=C3)C=C2
• CAS Number: 1802148-05-5
• Cell Research: Cellular potency is studied using the DPP1-expressing monocytic U937 cell line. Briefly, cells grown in RPMI are plated on 384-well polypropylene v-bottom plates at a density of 5x10^5 cells/mL per well. Added to this is 10uL of AZD7986 at 37 degree C for 60 min, followed by 350uM Gly-Phe-AFC. The well fluorescence is read using a multilabel plate reader. Data are analyzed to calculate pIC50 values.
• Kinase Assay: Activation of neutrophil serine proteases is assessed in vitro using primary bone marrow-derived CD34+ neutrophil progenitor cells. Cells are cultured in media supplemented with rhSCF and rhIL-3 for 7 days, and then for a further 7 days in the presence of G-CSF and different concentrations of AZD7986 (38pM to 10uM). After harvesting and lysis with 10% Triton X-100 buffer, cell lysates are kept at -20 degree C until NSP activity analysis.
• In Vitro: AZD7986 shows good stability in plasma, with a half-life of >10 hours. AZD7986 inhibits activation of Pr3 and NE, but not CatG, in bone marrow cell lysates in a dose-dependent manner in vivo.
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for AZD7986, inhibitor

AZD7986 is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively).

Product Categories/Family for AZD7986, inhibitor

Proteases/Proteasome; Proteasome

References

Doyle K, et al. Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). J Med Chem. 2016 Oct 27;59(20):9457-9472.