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Neutrophil elastase inhibitor 4

Cat. No. M42348
Neutrophil elastase inhibitor 4 Structure
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Biological Activity

Neutrophil elastase inhibitor 4 is a competitive human neutrophil elastase (HNE) inhibitor (IC50: 42.30 nM, Ki: 8.04 nM).

Chemical Information
Molecular Weight 383.4
Formula C20H21N3O5
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] Weifeng Yao et al. Oxid Med Cell Longev. Neutrophil Elastase Inhibitors Suppress Oxidative Stress in Lung during Liver Transplantation

[2] Wendong Hao et al. J Immunol Res. Expressions of MMP-12, TIMP-4, and Neutrophil Elastase in PBMCs and Exhaled Breath Condensate in Patients with COPD and Their Relationships with Disease Severity and Acute Exacerbations

[3] Eduardo F P Ruivo et al. ChemMedChem. Clickable 4-Oxo-β-lactam-Based Selective Probing for Human Neutrophil Elastase Related Proteomes

[4] Masaaki Harada et al. Gen Thorac Cardiovasc Surg. A neutrophil elastase inhibitor improves lung function during ex vivo lung perfusion

[5] C Boudier et al. Biochem J. Oxidized mucus proteinase inhibitor: a fairly potent neutrophil elastase inhibitor

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