1. Metabolic Enzyme/Protease
  2. Elastase
  3. Freselestat quarterhydrate

Freselestat quarterhydrate (Synonyms: ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate)

Cat. No.: HY-15652A
Handling Instructions

Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity.

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

Freselestat quarterhydrate Chemical Structure

Freselestat quarterhydrate Chemical Structure

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5 mg USD 470 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity[1][2][3][4].

IC50 & Target

Ki: 12.2 nM (Neutrophil elastase)[3]

In Vitro

Simulated extracorporeal circulation is established by recirculating fresh heparinized (3.75 U/mL) human blood for 120 minutes in a membrane oxygenator and a roller pump with and without 1.0 μM of Freselestat (ONO-6818). Neutrophil elastase levels are significantly lower in the Freselestat group. Freselestat significantly reduces interleukin 8 and C5b-9 production. Freselestat does not modulate changes of CD11b and L-selectin during recirculation[3].

In Vivo

Freselestat (ONO-6818; 10-100 mg/kg; oral administration; daily; for 8 weeks) treatment attenuates dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid. ONO-6818 inhibits acute lung injury induced by HNE by minimizing lung hemorrhage and accumulation of neutrophils in the lung[1].

Animal Model: Male Wistar rats (228 g) induced by human neutrophil elastase (HNE)[1]
Dosage: 10 mg/kg, 100 mg/kg
Administration: Oral administration; daily; for 8 weeks
Result: Attenuated dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid.
Molecular Weight

457.03

Formula

C₂₃H₂₈N₆O₄.₁/₄H₂O

SMILES

O=C(NC(C(C1=NN=C(C(C)(C)C)O1)=O)C(C)C)CN(C(C2=CC=CC=C2)=NC=C3N)C3=O.[1/4].O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

Freselestat quarterhydrateONO-6818 quarterhydrateONO-PO-736 quarterhydrateElastaseNon-peptidicorallyneutrophilelastaseIL-8C5b-9myeloperoxidaseanti-inflammatoryInhibitorinhibitorinhibit

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Freselestat quarterhydrate
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