AZD7986 is a second generation reversible covalent, potent and selective DPP1 inhibitor potentially for the treatment of chronic obstructive pulmonary disease (COPD) with predicted human PK properties suitable for once daily human dosing.
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HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
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Accessible (Haz class 3, 4, 5 or 8), International
Brensocatib acts as an inhibitor of DPP1, exhibiting pIC50 values of 6.85, 7.6, 7.7, 7.8, and 7.8 across various species—human, mouse, rat, dog, and rabbit, respectively. Brensocatib demonstrates stability in the propionaldehyde reactivity assay, maintaining a half-life exceeding 50 hours. When cells are differentiated in the presence of Brensocatib, ranging from 38 pM to 10 μM, a notable reduction in enzyme activity within cell lysates is observed for DPP1 and the three neutrophil serine proteases (NSPs)—NE, Pr3, and CatG. Brensocatib effectively suppresses the activation of these NSPs in a dose-responsive manner, with pIC50 values approximating 7 for each. At a concentration of 10 μM Brensocatib, the activity levels of NE, Pr3, and CatG are significantly diminished, dropping to 4 to 10% of the baseline control[1].
Brensocatib 动物研究
Animal study
Brensocatib exhibits commendable stability in plasma, maintaining a half-life of over 10 hours. In vivo, Brensocatib selectively inhibits the activation of NE and Pr3 in a dose-dependent fashion within bone marrow cell lysates, while CatG activation remains unaffected[1].
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