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Technical Data
| Formula | C17H12Br2O3 |
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| Molecular Weight | 424.08 | CAS No. | 3562-84-3 | |
| Solubility (25°C)* | In vitro | DMSO | 85 mg/mL (200.43 mM) | |
| Ethanol | 15 mg/mL (35.37 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | Benzbromarone(Desuric) is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM. | ||
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| In vitro | Benzbromarone (20 μM) decreases mitochondrial membrane potential by 81% in isolated rat hepatocytes. Benzbromarone decreases state 3 oxidation and respiratory control ratios for L-glutamate with IC50 < 1 μM in isolated rat liver mitochondria. Benzbromarone (50 μM) uncouples oxidative phosphorylation and increases oxygen consumption by hepatocytes starting at 10 μM in isolated rat hepatocytes. Benzbromarone also inhibits the formation of acid-soluble β-oxidation products in a dose-dependent manner with IC50 of 2 μM. Benzbromarone (100 μM) inhibits the electron transport chain and are uncouplers of oxidative phosphorylation in isolated rat liver mitochondria. Benzbromarone (1 μM) leads to concentration-dependent increasion of ROS production in HepG2 cells. Benzbromarone (100 μM) leads to a significant increase in mitochondrial size of isolated rat liver mitochondria. Benzbromarone is associated with leakage of cytochrome c into the cytoplasm of HepG2 cells. Benzbromarone (100 μM) results in the proportion of apoptotic cells of 11% in rat hepatocytes. [2] Benzbromarone significantly reduces the oxypurinol uptake at a concentration as low as 10 nM and completely blocks it at 1 μM. Benzbromarone (1 μM) uptakes the typical substrate of OCTN1 (tetraethylammonium) and OCTN2 (carnitine) in the HEK293 cells expressed with human OCTN1 by 96.7% and 111% of control, respectively. [3] Benzbromarone completely inhibits urate uptake at 50 μM in URAT1-expressing oocytes, with IC50 of less than 0.1 μM. [4] Benzbromarone activates through sequential hydroxylation of the benzofuran ring to a catechol, which can then be further oxidized to a reactive quinone intermediate capable of adducting protein. [5] |
Protocol (from reference)
References
Selleck's Benzbromarone has been cited by 1 publication
| Drug repositioning as a therapeutic strategy for neurodegenerations associated with OPA1 mutations [ Hum Mol Genet, 2020, ddaa244] | PubMed: 33231680 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.