2. Metabolic Enzyme/Protease
  3. Elastase
  4. Freselestat

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

Cat. No.: HY-15652 Purity: 99.00%
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Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat 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 has a potent anti-inflammatory activity.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Freselestat quarterhydrate) usually boasts enhanced water solubility and stability.

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

Freselestat Chemical Structure

Freselestat Chemical Structure

CAS No. : 208848-19-5

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Freselestat Related Antibodies

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Description

Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat 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 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].

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

Freselestat Related Antibodies
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].

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

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

452.51

Formula

C23H28N6O4
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (220.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2099 mL 11.0495 mL 22.0990 mL
5 mM 0.4420 mL 2.2099 mL 4.4198 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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=
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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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(per animal)

g

Dosing volume
(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2099 mL 11.0495 mL 22.0990 mL 55.2474 mL
5 mM 0.4420 mL 2.2099 mL 4.4198 mL 11.0495 mL
10 mM 0.2210 mL 1.1049 mL 2.2099 mL 5.5247 mL
15 mM 0.1473 mL 0.7366 mL 1.4733 mL 3.6832 mL
20 mM 0.1105 mL 0.5525 mL 1.1049 mL 2.7624 mL
25 mM 0.0884 mL 0.4420 mL 0.8840 mL 2.2099 mL
30 mM 0.0737 mL 0.3683 mL 0.7366 mL 1.8416 mL
40 mM 0.0552 mL 0.2762 mL 0.5525 mL 1.3812 mL
50 mM 0.0442 mL 0.2210 mL 0.4420 mL 1.1049 mL
60 mM 0.0368 mL 0.1842 mL 0.3683 mL 0.9208 mL
80 mM 0.0276 mL 0.1381 mL 0.2762 mL 0.6906 mL
100 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5525 mL
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Freselestat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Freselestat208848-19-5ONO-6818 ONO-PO-736ONO6818ONO 6818ElastaseNon-peptidicorallyneutrophilelastaseIL-8C5b-9myeloperoxidaseanti-inflammatoryInhibitorinhibitorinhibit

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