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Brensocatib

Catalog No. TQ0038   CAS 1802148-05-5
Synonyms: AZD7986, INS 1007

Brensocatib (AZD7986) is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Brensocatib Chemical Structure
Brensocatib, CAS 1802148-05-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 67.00
5 mg In stock $ 163.00
10 mg In stock $ 288.00
25 mg In stock $ 485.00
50 mg In stock $ 693.00
1 mL * 10 mM (in DMSO) In stock $ 178.00
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Purity: 99.05%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Brensocatib (AZD7986) is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively).
Targets&IC50 DPP1:pIC50: 6.85(human), DPP1:pIC50: 7.6(mouse), DPP1:pIC50: 7.7(rat), DPP1:pIC50: 7.8(dog), DPP1:pIC50: 7.8(rabbit)
In vitro AZD7986 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.
In vivo AZD7986 shows good stability in plasma, with a half-life of >10 h. AZD7986 inhibits activation of Pr3 and NE, but not CatG, in bone marrow cell lysates in a dose-dependent manner in vivo.
Kinase Assay Activation of neutrophil serine proteases 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 Research 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 5×10^5 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.
Animal Research Rats are used for the in vivo study. Naive rats are dosed orally twice daily with AZD7986 at 0.2, 2, and 20 mg/kg/day for 8 days. At termination, bone marrow is taken by femural aspiration for neutrophil serine proteases activity analysis using commercial synthetic peptide substrates.
Synonyms AZD7986, INS 1007
Molecular Weight 420.46
Formula C23H24N4O4
CAS No. 1802148-05-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: ≥100 mg/mL (237.83 mM)

H2O: Insoluble

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
NO PAINS Compound Library HIF-1 Signaling Pathway Compound Library Ubiquitination Compound Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Drug Repurposing Compound Library Orally Active Compound Library Clinical Compound Library

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Keywords

Brensocatib 1802148-05-5 Proteases/Proteasome Ubiquitination Proteasome Dipeptidyl Peptidase AZD 7986 AZD-7986 INS1007 DPP inhibit AZD7986 INS 1007 INS-1007 Inhibitor inhibitor

 

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