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Brensocatib

Cat. No. M14317
Brensocatib Structure
Synonym:

AZD7986; INS 1007

Size Price Availability Quantity
5mg USD 198  USD198 In stock
10mg USD 345  USD345 In stock
50mg USD 1180  USD1180 In stock
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Quality Control & Documentation
Biological Activity

Brensocatib (AZD7986) is an oral 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.

Chemical Information
Molecular Weight 420.46
CAS Number 1802148-05-5
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Xiao Bao Shen, et al. Cathepsin C inhibitors as anti-inflammatory drug discovery: Challenges and opportunities

[2] Robert Palmr, et al. Dipeptidyl Peptidase 1 Inhibitor AZD7986 Induces a Sustained, Exposure-Dependent Reduction in Neutrophil Elastase Activity in Healthy Subjects

[3] James D Chalmers, et al. Phase 2 Trial of the DPP-1 Inhibitor Brensocatib in Bronchiectasis

[4] Lijuan Sun, et al. Activating a collaborative innate-adaptive immune response to control metastasis

[5] Daniela F Quail, et al. Neutrophil phenotypes and functions in cancer: A consensus statement

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Keywords: Brensocatib, AZD7986; INS 1007 supplier, DPP-4, inhibitors, activators

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