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

Cat. No.: HY-15652A Purity: ≥99.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a K_i 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

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5 mg	USD 470	Ask For Quote & Lead Time

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Other Forms of Freselestat quarterhydrate:

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Biological Activity
Purity & Documentation
References
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Description

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.

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
10 mM	0.2188 mL	1.0940 mL	2.1880 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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

Purity: ≥99.0%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (254 KB) Elemental Analysis Report (112 KB)

Handling Instructions (2659 KB)

References

[1]. Am J Respir Crit Care Med. 2002 Aug 15;166(4):496-500. [Content Brief]

[2]. K Ohmoto, et al. Design and synthesis of new orally active inhibitors of human neutrophil elastase. Bioorg Med Chem. 2001 May;9(5):1307-23. [Content Brief]

[3]. Yasushi Hirota, et al. Effects of the neutrophil elastase inhibitor (ONO-6818) on acetic acid induced colitis in Syrian hamsters. J Vet Med Sci. 2004 Oct;66(10):1223-8. [Content Brief]

[4]. Yukihiro Yoshimura, et al. ONO-6818, a novel, potent neutrophil elastase inhibitor, reduces inflammatory mediators during simulated extracorporeal circulation. Ann Thorac Surg. 2003 Oct;76(4):1234-9. [Content Brief]

Complete Stock Solution Preparation Table

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

Freselestat quarterhydrate Related Classifications

Inflammation/Immunology

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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