| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Furegrelate sodium targets thromboxane A2 synthase (TXA2 synthase), a key enzyme in the arachidonic acid cascade that converts prostaglandin H2 to thromboxane A2. By inhibiting this enzyme, it reduces thromboxane A2 production, leading to vasodilation and inhibition of platelet aggregation.
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| ln Vitro |
In vitro, Furegrelate sodium is a potent and selective inhibitor of thromboxane A2 synthase. It inhibits the production of thromboxane A2 in platelet and vascular preparations. Its activity makes it a valuable tool for studying the role of thromboxane A2 in cardiovascular physiology and disease.
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| ln Vivo |
Furegrelate Sodium (1–5 mg/kg; IV) inhibits the aggregation of blood vessels brought on by a constricted coronary artery [1]. Intravenous furegrelate sodium (0.1–5 mg/kg) inhibits blood vessel aggregation brought on by constricted coronary arteries [1]. keeps the pulmonary artery structure intact, which prevents the development of hypoxia-induced pulmonary arterial hypertension (PAH) in newborn pigs [2]. Furegrelate has a strong affinity for target enzymes and a prolonged half-life when compared to a number of other medications for the treatment of PAH, such as zinc monoxide and antagonist cycline analogs [2].
In vivo, Furegrelate sodium has been studied for its potential in cardiovascular research. As a TXA2 synthase inhibitor, it can be administered to animal models to study its effects on platelet aggregation, vasoconstriction, and thrombosis. Its ability to reduce thromboxane A2 production translates to in vivo efficacy. |
| Enzyme Assay |
In vitro enzyme assays for Furegrelate sodium involve measuring its inhibition of TXA2 synthase activity. The enzyme is incubated with increasing concentrations of the compound and prostaglandin H2 as substrate. The production of thromboxane B2 (the stable metabolite of TXA2) is measured by radioimmunoassay or ELISA. IC50 values are calculated from dose-response curves.
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| Cell Assay |
For in vitro cell-based assays, platelets or cells expressing TXA2 synthase are cultured and treated with Furegrelate sodium at various concentrations. Thromboxane B2 production is measured by ELISA. Platelet aggregation is assessed using aggregometry. Cell viability is assessed by standard assays.
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| Animal Protocol |
Animal/Disease Models: Mongrel dog (19-30 kg) [1]
Doses: 1-5 mg/kg Route of Administration: Oral (via gastric tube) Experimental Results: Prevention of coronary artery obstruction. In vivo animal studies with Furegrelate sodium are conducted in models of thrombosis and cardiovascular disease. The compound is administered orally or intraperitoneally to rodents. Platelet aggregation, thrombus formation, and vascular function are assessed. The compound's effects on thromboxane A2 production are measured in blood or tissues. |
| ADME/Pharmacokinetics |
Furegrelate sodium (CAS: 85666-17-7) has a molecular weight of 301.27 g/mol and a molecular formula of C14H12FNNaO3. Appearance: solid powder. Purity: ≥98%. Solubility: DMSO. Storage: -20°C. The compound is a potent and selective TXA2 synthase inhibitor.
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| Toxicity/Toxicokinetics |
Furegrelate sodium is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a TXA2 synthase inhibitor, it may have effects on platelet function and vascular tone. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
See also: Anagrelide Hydrochloride (related); Furegrelate (has active moiety).
Furegrelate sodium is a potent and selective inhibitor of thromboxane A2 synthase (TXA2 synthase). It inhibits thromboxane A2 production and has been studied for its potential in cardiovascular research. It is not FDA-approved and is intended for research use only. |
| Molecular Formula |
C15H10NNAO3
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|---|---|
| Molecular Weight |
275.2346
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| Exact Mass |
275.055
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| CAS # |
85666-17-7
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| Related CAS # |
Furegrelate;85666-24-6
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| PubChem CID |
23663954
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| Appearance |
White to light yellow solid powder
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| Boiling Point |
458.7ºC at 760 mmHg
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| Flash Point |
231.2ºC
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| LogP |
1.782
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
339
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CN=C1)CC2=CC3=C(C=C2)OC(=C3)C(=O)[O-].O.[Na+]
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| InChi Key |
XBTIPIZROJAKOJ-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C15H11NO3.Na/c17-15(18)14-8-12-7-10(3-4-13(12)19-14)6-11-2-1-5-16-9-11;/h1-5,7-9H,6H2,(H,17,18);/q;+1/p-1
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| Chemical Name |
sodium;5-(pyridin-3-ylmethyl)-1-benzofuran-2-carboxylate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~13 mg/mL (~47.23 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (6.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (6.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (6.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6333 mL | 18.1666 mL | 36.3332 mL | |
| 5 mM | 0.7267 mL | 3.6333 mL | 7.2666 mL | |
| 10 mM | 0.3633 mL | 1.8167 mL | 3.6333 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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