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Brensocatib(AZD7986)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Brensocatib(AZD7986)图片
CAS NO:1802148-05-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 420.47
Formula C23H24N4O4
CAS No. 1802148-05-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:> 10 mM
Water: N/A
Ethanol: N/A
Chemical Name (S)-N-((S)-1-cyano-2-(4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide
Synonyms Brensocatib; INS 1007; AZD7986; INS-1007; AZD-7986; INS1007; AZD 7986
实验参考方法
In Vitro

In vitro activity: AZD7986 (formerly known as INS 1007) is a novel, second generation, highly potent, reversible, and selective DPP1 (Dipeptidyl peptidase 1) inhibitor pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively. It has the potential for COPD (chronic obstructive pulmonary disease) treatment with predicted human PK properties suitable for once daily human dosing.


Kinase Assay: Activation of neutrophil serine proteases (NSPs) 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 (38 pM to 10 μM). After harvesting and lysis with 10% Triton X-100 buffer, cell lysates are kept at -20°C until NSP activity analysis.


Cell Assay: 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 5×105 cells/mL per well. Added to this is 10 μL of AZD7986 at 37°C for 60 min, followed by 350 μM Gly-Phe-AFC. The well fluorescence is read using a multilabel plate reader. Data are analyzed to calculate pIC50 values.

In Vivo AZD7986 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.
Animal model Naive rats
Formulation & Dosage 0.2, 2, and 20 mg/kg/day; oral
References J Med Chem. 2016 Oct 27;59(20):9457-9472.