Brensocatib

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 In Vitro Results from cell assay show that Brensocatib (AZD7986) is a 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. 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 pIC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:DPP-1

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