Keywords

• AZD7986
• AZD 7986
• AZD-7986

Quick Details

• ProName: AZD7986
• CasNo: 1802148-05-5
• Molecular Formula: C??H??N?O?
• Appearance: yellow powder
• Application: AZD7986 is a DPP1 inhibitor
• ProductionCapacity: Gram/Day
• Purity: 98%
• LimitNum: 1 Gram

Superiority

AZD7986 is a DPP1 inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively.

In Vitro

AZD7986 is a DPP1 inhibitor with pIC₅₀s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively. AZD7986 (Compound 30) is stable in the propionaldehyde reactivity assay, with a half-life over 50 h. After differentiation in the presence of AZD7986 (38 pM to 10 μM), concentration-dependent decreases in cell lysate enzyme activity are observed for DPP1, as well as for all of the three NSPs, NE, Pr3, and CatG. AZD7986 inhibits activation of all three NSPs in a concentration dependent manner, with pIC₅₀ values of around 7 for all three NSPs. The reduction of the activities is almost complete, with NE, Pr3, and CatG activities reduced to 4 to 10% of control at 10 μM AZD7986^[1].

In Vivo

AZD7986 (Compound 30) shows good stability in plasma, with a half life of >10 h. AZD7986 inhibits activation of NE and Pr3, but not CatG, in bone marrow cell lysates in a dose dependent manner in vivo^[1].

[1]. 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.

Details