Brensocatib (AZD7986) 是一个二肽基肽酶 1 (DPP1) 抑制剂，在人，小鼠，大鼠，狗和兔中的 pIC₅₀ 值分别为 6.85, 7.6, 7.7, 7.8 和 7.8。

Brensocatib (AZD7986) is an oral dipeptidyl peptidase 1 (DPP1) inhibitor with pIC 50 s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively.

Solid

pIC50: 6.85 (human DPP1), 7.6 (mouse DPP1), 7.7 (rat DPP1), 7.8 (dog DPP1), 7.8 (rabbit DPP1)

Results from cell assay show that Brensocatib (AZD7986) is a Dipeptidyl peptidase 1 (DPP1) inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively. Brensocatib is stable in the propionaldehyde reactivity assay, with a half-life over 50 h. After differentiation in the presence of Brensocatib (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. Brensocatib 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 Brensocatib. has not independently confirm

Brensocatib (AZD7986) shows good stability in plasma, with a half life of >10 h. Brensocatib inhibits activation of NE and Pr3, but not CatG, in bone marrow cell lysates in a dose dependent manner in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 100 mg/mL (237.83 mM)配制储备液