1. Metabolic Enzyme/Protease
  2. Elastase
  3. BAY-85-8501

BAY-85-8501 

Cat. No.: HY-19908 Purity: 99.59%
Handling Instructions

BAY-85-8501 is a selective, reversible 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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of BAY-85-8501:

Top Publications Citing Use of Products

Publications Citing Use of MCE BAY-85-8501

    BAY-85-8501 purchased from MCE. Usage Cited in: Chinese Academy of Sciences. 2019 Aug.

    Blood from 3 healthy individuals, was separated using Lymhoprep, neutrophils isolated and plated out in 96 well plates at 5x105 and incubated with PMA (50 nM) for 3 hours, with and without inhibitor as above. Results show that BAY-85-8501 inhibits human neutrophil elastase at all 3 concentrations (50, 25, and 12.5 µM) with a significance of P<0.0001, when compared to the positive control of human neutrophil elastase and cells incubated with PMA and vehicle.
    • Biological Activity

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    Description

    BAY-85-8501 is a selective, reversible 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
    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    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
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    Keywords:

    BAY-85-8501ElastaseInhibitorinhibitorinhibit

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    Product name:
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    Cat. No.:
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