Elastases

Elastase inhibitors block serine proteases that degrade elastin and other extracellular matrix proteins. Neutrophil elastase, the main target here, is stored in azurophil granules of neutrophils together with proteinase 3 and cathepsin G. After release it cleaves elastin and collagens, and it processes cytokines and cell surface receptors at sites of inflammation. During the formation of neutrophil extracellular traps (NETs), the enzyme moves to the nucleus and helps to decondense chromatin. Inhibitors are used in models of acute lung injury, cystic fibrosis and chronic obstructive pulmonary disease (COPD). Sivelestat, BAY-678 and DMP 777 are inhibitors of human neutrophil elastase. Related enzymes of the same class are listed under Serine Protease.

Items 1-25 of 48

  • Sivelestat sodium salt
    Cat. No.
    A14073

    Sivelestat sodium salt

    Synonyms: ONO-5046

    Sivelestat sodium salt is a selective leukocyte elastase inhibitor (IC50 = 44 nM) that displays no activity at a range of other proteases. It inhibits NF-kB activation and LTB4-induced neutrophil transmigration in vitro.

    2 mg
    $25.00
    5 mg
    $50.00
    All 6 sizes
  • DMP 777
    Cat. No.
    A11390

    DMP 777

    Synonyms: L-694458

    DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.

    2 mg
    $90.00
    5 mg
    $155.00
    All 7 sizes
  • ZD-0892
    Cat. No.
    A13303

    ZD-0892

    ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.

    1 mg
    $110.00
    5 mg
    $285.00
    All 6 sizes
  • Sivelestat
    Cat. No.
    A14184

    Sivelestat

    Synonyms: Elastase Inhibitor IV

    Sivelestat is a cell-permeable sulfanilide compound that acts as a potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC50 = 19-49 nM in rat, rabbit, hamster, human, and mouse leukocyte elastase).

    5 mg
    $35.00
    10 mg
    $55.00
    All 8 sizes
  • SSR 69071
    Cat. No.
    A15315

    SSR 69071

    SSR 69071 is a high affinity, potent inhibitor of Neutrophil Elastase (human leukocyte elastase, HLE) (IC50 = 3.9 nM).

    1 mg
    $45.00
    5 mg
    $170.00
    All 4 sizes
  • BAY-678
    Cat. No.
    A16866

    BAY-678

    BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

    5 mg
    $30.00
    10 mg
    $50.00
    All 7 sizes
  • N-Acetylglucosamine
    Cat. No.
    A17841

    N-Acetylglucosamine

    Synonyms: Acetylglucosamine; GlcNAc; Bio-NAG; GreenNAG; Marine Sweet; N-Acetyl-D-glucosamine; NSC 400525; NSC 524344.

    Acetylglucosamine or N-acetylglucosamine is potentially for the treatment of irritable bowel syndrome. N-Acetylglucosamine (GlcNAc) is a monosaccharide that usually polymerizes linearly through (1,4)-β-linkages. GlcNAc has been reported to be an inhibitor of elastase release from human polymorphonuclear leukocytes (range 8–17% inhibition), however this is much weaker than the inhibition seen with N-acetylgalactosamine (range 92–100%).

    1 g
    $25.00
    5 g
    $75.00
    All 3 sizes
  • BAY-678 racemate
    Cat. No.
    A19564

    BAY-678 racemate

    BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

    5 mg
    $500.00
    10 mg
    $800.00
    All 5 sizes
  • BAY-677
    Cat. No.
    A19838

    BAY-677

    BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM.

    2 mg
    $30.00
    5 mg
    $65.00
    All 6 sizes
  • Lodelaben
    Cat. No.
    A20510

    Lodelaben

    Synonyms: SC-39026; Declaben

    Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.

    1 mg
    $920.00
    5 mg
    $2,280.00
    All 4 sizes
  • BAY-85-8501
    Cat. No.
    A20645

    BAY-85-8501

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

    1 mg
    $80.00
    2 mg
    $125.00
    All 8 sizes
  • AE-3763
    Cat. No.
    A20788

    AE-3763

    AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM.

    1 mg
    $315.00
    5 mg
    $375.00
    All 6 sizes
  • GW311616
    Cat. No.
    A22033

    GW311616

    GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM.

    1 mg
    $480.00
    5 mg
    $1,260.00
    All 3 sizes
  • JCP174
    Cat. No.
    A22107

    JCP174

    JCP174 is a depalmitoylase inhibitor that enhances Toxoplasma host-cell invasion by targeting TgPPT1.

    1 mg
    $85.00
    5 mg
    $225.00
    All 8 sizes
  • Elastase-IN-3
    Cat. No.
    A46466

    Elastase-IN-3

    Elastase-IN-3 is a potent inhibitor of elastase, an enzyme produced by Pseudomonas aeruginosa. By specifically targeting the LasR protein with a KD value of 7.04 µM, Elastase-IN-3 disrupts the quorum sensing system, thereby inhibiting the bacterial communication crucial for virulence and biofilm formation. This compound has significant applications in biodefense, food safety, and antibacterial research, particularly in studying the impact of Pseudomonas aeruginosa on food spoilage and related infections.

    1 g
    $20.00
    5 g
    $35.00
    All 6 sizes
  • Neltenexine
    Cat. No.
    A66450

    Neltenexine

    Neltenexine is a potent elastase inhibitor that reduces anion secretion in bronchial epithelial cells. It achieves this by inhibiting chloride and bicarbonate uptake through the Na+/K+/2Cl- and Na+/HCO3- cotransporters, while not affecting the CFTR channel. Additionally, it can stimulate the chloride/bicarbonate exchanger, contributing to its mucolytic effects. Research indicates that Neltenexine effectively prevents pulmonary emphysema and reduces alveolar deformation in elastase-induced rat models, making it a valuable tool for studying lung diseases such as chronic obstructive pulmonary disease (COPD).

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • GW311616 hydrochloride
    Cat. No.
    A71026

    GW311616 hydrochloride

    Synonyms: GW311616A

    GW311616 hydrochloride is a selective inhibitor of human neutrophil elastase (HNE), demonstrating potent activity with an IC50 value of 22 nM and a Ki value of 0.31 nM. This compound exhibits oral bioavailability and extended duration of action, making it a valuable tool for studying the role of HNE in various inflammatory diseases. Research applications include the investigation of HNE's involvement in tissue remodeling and acute lung injury.

    1 mg
    $230.00
    5 mg
    $370.00
    All 4 sizes
  • FK706
    Cat. No.
    A71028

    FK706

    FK706 is a potent competitive inhibitor of human neutrophil elastase, exhibiting an IC50 of 83 nM and a Ki of 4.2 nM. This compound effectively inhibits both mouse neutrophil elastase and porcine pancreatic elastase, with IC50 values of 22 nM and 100 nM, respectively. Importantly, FK706 shows selectivity by not inhibiting other serine proteinases, including human pancreatic trypsin and α-chymotrypsin. Due to its anti-inflammatory properties, FK706 is valuable for research related to inflammatory diseases and conditions associated with elastase activity.

    5 mg
    $385.00
    10 mg
    $630.00
    All 5 sizes
  • Neutrophil elastase inhibitor 1
    Cat. No.
    A71030

    Neutrophil elastase inhibitor 1

    Neutrophil elastase inhibitor 1 is a competitive, pseudoirreversible inhibitor primarily targeting neutrophil elastase. With an IC50 value of 7 nM, it effectively modulates elastase activity, making it a valuable tool in the study of inflammatory diseases where neutrophil activation plays a crucial role. This compound can facilitate research into therapeutic interventions for conditions characterized by excessive elastase activity.

    5 mg
    $125.00
    10 mg
    $235.00
    All 2 sizes
  • (R)-BAY-85-8501
    Cat. No.
    A71031

    (R)-BAY-85-8501

    (R)-BAY-85-8501 is the less active enantiomer of BAY-85-8501, a selective and potent inhibitor of Human Neutrophil Elastase (HNE) with an IC50 of 65 pM. This compound is utilized in research to investigate the role of HNE in various inflammatory conditions and to explore therapeutic strategies targeting this enzyme. Its specific inhibitory action makes it a valuable tool for studying neutrophil function and related diseases.

    5 mg
    $370.00
    10 mg
    $565.00
    All 5 sizes
  • Lonodelestat
    Cat. No.
    A71033

    Lonodelestat

    Synonyms: POL6014

    Lonodelestat is a selective, orally active peptide inhibitor of human neutrophil elastase (hNE). This compound exhibits significant potential for the study of cystic fibrosis (CF) by modulating the activity of hNE, a key enzyme implicated in inflammatory responses and tissue damage in CF patients. It serves as a valuable tool for investigating therapeutic strategies aimed at mitigating the effects of excessive neutrophil activity in pulmonary diseases.

    5 mg
    $245.00
    10 mg
    $380.00
    All 3 sizes
  • ZD8321
    Cat. No.
    A71034

    ZD8321

    ZD8321 is a potent inhibitor of human neutrophil elastase (NE), demonstrating an inhibition constant (Ki) of 13±1.7 nM. This compound effectively modulates elastase activity, making it valuable in research focused on inflammatory diseases and tissue remodeling. ZD8321 is suitable for studies investigating the role of elastase in various pathological conditions and therapeutic interventions.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

Items 1-25 of 48

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