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Furegrelate (sodium salt) (Synonyms: U-63557A)

Catalog No.GC13536

Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor.

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Furegrelate (sodium salt) Chemical Structure

Cas No.: 85666-17-7

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10mM (in 1mL DMSO)
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5mg
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10mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

Description of Furegrelate (sodium salt)

Furegrelate (sodium salt) is a potent inhibitor of thromboxane synthase [1][2].

Thromboxane A synthase 1 (platelet, cytochrome P450, family 5, subfamily A) is a cytochrome P450 enzyme that catalyzes the conversion of prostaglandin H2 to thromboxane A2. Thromboxanes play an important role in vasoconstriction and platelet aggregation.

Furegrelate (sodium salt), also known as sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate (U-63557A), is a potent, specific and orally available thromboxane synthase inhibitor. U-63557A is a potent inhibitor of the thromboxane synthase in human platelets in vitro, as well as in rhesus monkey platelets ex vivo. U-63557A didn’t inhibit thrombin-stimulated PGI2 biosynthesis in human endothelial cells, the 5-lipoxygenase in human neutrophils, or the cyclooxygenase in a variety of test systems [2].

In rhesus monkeys, U-63557A inhibited the platelet thromboxane synthase by approximately 80% for at least 12 hrs. In anesthetized dogs, U-63557A inhibited the blockage of stenosed coronary arteries caused platelet aggregation. While the protective effects of U-63557A could be reversed by cyclooxygenase inhibitors. U-63557A is a promising compound for the evaluation of the role of thromboxane synthase in a variety of pathophysiological states [2].

References:
[1].  Johnson RA, Nidy EG, Aiken JW, et al. Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids. J Med Chem. 1986 Aug;29(8):1461-8.
[2].  Gorman RR, Johnson RA, Spilman CH, et al. Inhibition of platelet thromboxane A2 synthase activity by sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate. Prostaglandins. 1983 Aug;26(2):325-42.

Chemical Properties of Furegrelate (sodium salt)

Cas No. 85666-17-7 SDF
Synonyms U-63557A
Chemical Name 5-(3-pyridinylmethyl)-2-benzofurancarboxylic acid, sodium salt
Canonical SMILES O=C(C1=CC2=C(O1)C=CC(CC3=CN=CC=C3)=C2)[O-].[Na+]
Formula C15H10NO3 • Na M.Wt 275.2
Solubility ≤15mg/ml in Water Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Furegrelate (sodium salt)

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1 mg 5 mg 10 mg
1 mM 3.6337 mL 18.1686 mL 36.3372 mL
5 mM 0.7267 mL 3.6337 mL 7.2674 mL
10 mM 0.3634 mL 1.8169 mL 3.6337 mL
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In vivo Formulation Calculator (Clear solution) of Furegrelate (sodium salt)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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