1. Metabolic Enzyme/Protease
  2. Elastase

BAY-85-8501 

Cat. No.: HY-19908
Handling Instructions

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

For research use only. We do not sell to patients.

BAY-85-8501 Chemical Structure

BAY-85-8501 Chemical Structure

CAS No. : 1161921-82-9

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 65 pM (HNE)[1].

In Vivo

In this model the exogenous HNE noxa is the primary cause of injury and lung hemorrhage. Based on picomolar potency against HNE as well as single digit potency versus MNE, BAY-85-8501 (29) completely prevents the development of lung injury and subsequent inflammation when administered 1 h prior to the HNE noxa. In the 0.01 mg/kg dose group, hemoglobin concentration is already significantly decreased. At a dose of 0.1 mg/kg, a significant effect on neutrophil count is observed. In this setup, efficacy is predominantly driven by potency against HNE (Ki=0.08 nM). As the highly HNE-selective inhibitor BAY 85-8501 has no effect on PPE, BAY-85-8501 could not prevent the primary lung injury in this setup. Nevertheless, BAY-85-8501 could inhibit MNE, the endogenous driver of inflammation and secondary injury, although with decreased potency. Consequently, the effects of BAY-85-8501 on inflammation and secondary injury are weaker at this point, and only observed at 30-fold higher doses. Efficacy is predominantly driven by potency against MNE (Ki=6 nM) in this second setup[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1077 mL 10.5383 mL 21.0766 mL
5 mM 0.4215 mL 2.1077 mL 4.2153 mL
10 mM 0.2108 mL 1.0538 mL 2.1077 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Elastaseinduced lung failure in mice, rats or hamsters is a widely used animal model of acute lung failure. The animals are treated 1 hour prior to orotracheal instillation of human neutrophil elastase (HNE) or porcine pancreatic elastase (PPE). In this study, each mouse receives BAY-85-8501 with different concentrations (0.003, 0.01, 0.03, 0.1, 0.3, 3, 10, 30 mg/kg) by P.O.[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

474.46

Formula

C₂₂H₁₇F₃N₄O₃S

CAS No.

1161921-82-9

SMILES

N#CC1=C(C)N(C2=CC=CC(C(F)(F)F)=C2)C(N(C)[[email protected]@H]1C3=CC=C(C#N)C=C3S(=O)(C)=O)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BAY-85-8501
Cat. No.:
HY-19908
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BAY-85-8501

Cat. No.: HY-19908