| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Benzbromarone (L2214; L 2214; MJ-10061; MJ10061; L-2214; L2214-Labaz; Narcaricin; Normurat), an approved anti-gout drug (uricosuric drug) for the last 30 years, is a potent CYP2C9 inhibitor with Ki value of 19.3 nM. It also acts as non-competitive inhibitor of XO/xanthine oxidase. Benzbromarone is structurally related to the antiarrhythmic amiodarone and is highly effective and well tolerated, and clinical trials as early as 1981 and as recently as April 2008 have suggested it is superior to both allopurinol, a xanthine oxidase inhibitor but not uricosuric, and probenecid, another uricosuric drug.
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| ln Vivo |
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| Animal Protocol |
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| Toxicity/Toxicokinetics |
Hepatotoxicity
Liver test abnormalities have been reported to occur rarely during benzbromarone therapy, in only 0.1% of patients in clinical trials. Furthermore, it was used widely for many years without reports of hepatotoxicity until the late 1980s, after which several cases of acute liver injury and acute liver failure during benzbromarone therapy were published. Hepatic injury arises after 1 to 6 months of therapy presenting with jaundice and fatigue, usually with a hepatocellular pattern of enzyme elevations. Immunoallergic symptoms (rash, fever) are uncommon. Low levels of autoantibodies have been reported in some cases with liver histology demonstrating chronic active hepatitis, particularly if benzbromarone is not stopped promptly. Upon stopping therapy, resolution is typically within 1 to 3 months. The hepatic injury from benzbromarone is similar to that reported with benzarone, a structurally related drug that was used for peripheral vascular disease, but also withdrawn also because of concerns over hepatotoxicity. Likelihood score: B (highly likely but rare cause of clinically apparent liver injury). |
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| References |
Drug Metab Dispos.2003 Jul;31(7):967-71;Hepatology.2005 Apr;41(4):925-35.
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| Additional Infomation |
Benzbromarone is 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication. It has a role as a uricosuric drug. It is a member of 1-benzofurans and an aromatic ketone. It is functionally related to a 2,6-dibromophenol.
Benzbromarone has been used in trials studying the basic science and treatment of Heart Failure, Hyperuricemia, Chronic Kidney Disease, Abnormal Renal Function, and Gout and Asymptomatic Hyperuricemia. Benzbromarone is a nonpurine xanthine oxidase inhibitor used for the treatment of gout, but never approved for use in the United States because of concerns over reports of acute liver injury and deaths with its use. Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout. |
| Molecular Formula |
C17H12BR2O3
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| Molecular Weight |
424.08
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| Exact Mass |
421.915
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| CAS # |
3562-84-3
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| Related CAS # |
Benzbromarone-d5
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| PubChem CID |
2333
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
514.1±50.0 °C at 760 mmHg
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| Melting Point |
161 - 163ºC
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| Flash Point |
264.7±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.673
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| LogP |
6.64
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
405
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WHQCHUCQKNIQEC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12Br2O3/c1-2-13-15(10-5-3-4-6-14(10)22-13)16(20)9-7-11(18)17(21)12(19)8-9/h3-8,21H,2H2,1H3
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| Chemical Name |
(3,5-dibromo-4-hydroxyphenyl)(2-ethylbenzofuran-3-yl)methanone
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.90 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 20.8 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: 2.08 mg/mL (4.90 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (4.90 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 | 2.3580 mL | 11.7902 mL | 23.5805 mL | |
| 5 mM | 0.4716 mL | 2.3580 mL | 4.7161 mL | |
| 10 mM | 0.2358 mL | 1.1790 mL | 2.3580 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02790450 | Completed | Drug: Benzbromarone | Idiopathic Pulmonary Arterial Hypertension |
Medical University of Graz | October 2015 | Phase 2 |
| NCT02338323 | Completed | Drug: Febuxostat Drug: Benzbromarone |
Chronic Kidney Disease Hyperuricemia |
Shanghai 10th People's Hospital | January 2015 | Not Applicable |
| NCT03100318 | Completed | Drug: Larotrectinib Sulfate Procedure: Bone Scan |
Hyperuricemia With or Without Gout | Fuji Yakuhin Co., Ltd. | April 1, 2017 | Phase 3 |
| 444 | Recruiting | Drug: FYU-981 Drug: Benzbromarone |
Recurrent Glioma Refractory Glioma |
National Cancer Institute (NCI) |
August 23, 2017 | Phase 2 |
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