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BAY-85-8501

Catalog No. T12613L   CAS 1161921-82-9

BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE; IC50 of 65 pM)

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BAY-85-8501 Chemical Structure
BAY-85-8501, CAS 1161921-82-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 179.00
5 mg In stock $ 455.00
10 mg In stock $ 672.00
25 mg In stock $ 1,060.00
50 mg In stock $ 1,430.00
100 mg In stock $ 1,920.00
1 mL * 10 mM (in DMSO) In stock $ 490.00
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Purity: 98.63%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE; IC50 of 65 pM)
Targets&IC50 HNE:65 pM
In vivo In this study, the exogenous compound HNE noxa is identified as the primary cause of lung injury and hemorrhage. BAY-85-8501 (29), due to its picomolar potency against HNE and high effectiveness against MNE, completely prevents lung injury and subsequent inflammation if administered one hour before exposure to HNE noxa. Despite its high selectivity for HNE inhibition, BAY-85-8501 does not prevent primary lung injury caused by PPE since it has no effect on it. However, BAY-85-8501 can inhibit MNE, an endogenous promoter of inflammation and secondary lung injury, albeit with lower potency. The prevention of inflammation and secondary injury by BAY-85-8501 is less pronounced and requires doses 30 times higher than standard. Its effectiveness primarily relies on its ability to inhibit MNE (Ki=6 nM) in these cases. At a dosage of 0.01 mg/kg, a significant reduction in hemoglobin concentration is noted, and at 0.1 mg/kg, a notable decrease in neutrophil count is observed, indicating efficacy is largely dependent on its potency against HNE (Ki=0.08 nM) in this scenario.
Molecular Weight 474.46
Formula C22H17F3N4O3S
CAS No. 1161921-82-9

Storage

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

Solubility Information

DMSO: 200 mg/mL (421.53 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Von Nussbaum F, et al. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Inhibitor Library Covalent Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Compound Library Clinical Compound Library ReFRAME Related Library

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Keywords

BAY-85-8501 1161921-82-9 Proteases/Proteasome Serine Protease inhibit Elastase Inhibitor BAY 85 8501 BAY858501 inhibitor

 

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