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

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

Cat. No.: HY-15652A Purity: ≥99.0%
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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.

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

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

Freselestat quarterhydrate Chemical Structure

Freselestat quarterhydrate Chemical Structure

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Freselestat quarterhydrate Related Antibodies

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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].

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

Freselestat quarterhydrate 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

457.03

Formula

C23H28N6O4.1/4H2O
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.[1/4].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 : 40 mg/mL (87.52 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 2.1880 mL 10.9402 mL 21.8804 mL
5 mM 0.4376 mL 2.1880 mL 4.3761 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)

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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 2.1880 mL 10.9402 mL 21.8804 mL 54.7010 mL
5 mM 0.4376 mL 2.1880 mL 4.3761 mL 10.9402 mL
10 mM 0.2188 mL 1.0940 mL 2.1880 mL 5.4701 mL
15 mM 0.1459 mL 0.7293 mL 1.4587 mL 3.6467 mL
20 mM 0.1094 mL 0.5470 mL 1.0940 mL 2.7351 mL
25 mM 0.0875 mL 0.4376 mL 0.8752 mL 2.1880 mL
30 mM 0.0729 mL 0.3647 mL 0.7293 mL 1.8234 mL
40 mM 0.0547 mL 0.2735 mL 0.5470 mL 1.3675 mL
50 mM 0.0438 mL 0.2188 mL 0.4376 mL 1.0940 mL
60 mM 0.0365 mL 0.1823 mL 0.3647 mL 0.9117 mL
80 mM 0.0274 mL 0.1368 mL 0.2735 mL 0.6838 mL
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Freselestat quarterhydrate 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:

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

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