| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| ln Vitro |
In vitro activity: Kinase Assay: Cell Assay: Broxaldine (Brobenzoxaldine) exhibits potent anticlostridial activity against multiple Clostridium species. It inhibits the growth of Clostridium difficile (including ribotype 027, 014/020, and non-toxigenic strains) with minimum inhibitory concentration (MIC) values ranging from 0.5–2 μg/mL. It also shows inhibitory activity against other Clostridium species, including Clostridium perfringens (MIC: 1–2 μg/mL), Clostridium ramosum (MIC: 2 μg/mL), Clostridium innocuum (MIC: 2 μg/mL), and Clostridium symbiosum (MIC: 4 μg/mL) [2] - The compound demonstrates no significant inhibitory activity against a panel of Gram-positive (Staphylococcus aureus, Enterococcus faecalis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) non-clostridial bacteria at concentrations up to 32 μg/mL, indicating selective anticlostridial activity [2] |
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| ln Vivo |
In a clinical trial involving 30 leprosy patients (25 multibacillary, 5 paucibacillary), combination therapy with Broxaldine (Brobenzoxaldine) (100 mg twice daily) and broxyquinoline (250 mg twice daily) for 6 months resulted in clinical improvement. Among the 25 multibacillary patients, 20 showed significant improvement (reduction in skin lesions, nerve tenderness, and bacterial index), 3 showed moderate improvement, and 2 showed no improvement. All 5 paucibacillary patients achieved complete cure (resolution of skin lesions and negative bacterial index) [1] |
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| Cell Assay |
Anticlostridial susceptibility assay: Prepare serial dilutions of Broxaldine (Brobenzoxaldine) in appropriate growth media (e.g., Brucella broth supplemented with hemin and vitamin K1). Inoculate the diluted compound with Clostridium strains (final bacterial concentration: 5×10⁵ CFU/mL) into 96-well plates. Incubate the plates anaerobically at 37°C for 48 hours. Determine the MIC as the lowest concentration of Broxaldine (Brobenzoxaldine) that inhibits visible bacterial growth [2]
- Non-clostridial bacterial susceptibility assay: Perform the same serial dilution and inoculation steps as the anticlostridial assay, using non-clostridial Gram-positive and Gram-negative bacterial strains. Incubate aerobically or anaerobically (depending on bacterial requirements) at 37°C for 24–48 hours. Evaluate bacterial growth inhibition at concentrations up to 32 μg/mL to assess selectivity [2] |
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| Animal Protocol |
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| Toxicity/Toxicokinetics |
In a 6-month clinical trial, broxaldine (100 mg twice daily) was well tolerated in combination with bromoquinoline. No serious adverse reactions were reported; three patients experienced mild and transient gastrointestinal discomfort (nausea, bloating), which resolved without discontinuation of the drug [1].
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| References | |||
| Additional Infomation |
Broxaldine is an antimicrobial agent initially used in combination with the known antileprosy drug bromoquinoline to treat leprosy[1]. Leprosy is a chronic infectious disease caused by Mycobacterium leprae, which primarily affects the skin, peripheral nerves, and mucous membranes. The combination therapy of broxaldine and bromoquinoline was designed to enhance efficacy through potential synergistic antimicrobial effects[1]. The selective anticlostridium activity of broxaldine suggests that it holds promise as a lead compound for developing novel therapies for clostridium-associated infections, such as Clostridium difficile infection, which is a major cause of medically-associated diarrhea and colitis[2].
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| Molecular Formula |
C17H11BR2NO2
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|---|---|---|
| Molecular Weight |
421.08
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| Exact Mass |
418.916
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| Elemental Analysis |
C, 48.49; H, 2.63; Br, 37.95; N, 3.33; O, 7.60
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| CAS # |
3684-46-6
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| Related CAS # |
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| PubChem CID |
77262
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| Appearance |
White to off-white solid powder
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| Density |
1.692g/cm3
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| Boiling Point |
538.1ºC at 760 mmHg
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| Flash Point |
279.2ºC
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| Index of Refraction |
1.68
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| LogP |
5.287
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| Hydrogen Bond Donor Count |
0
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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 |
400
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=NC2=C(OC(C3=CC=CC=C3)=O)C(Br)=CC(Br)=C2C=C1
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| InChi Key |
IJTPLVAAROHGGB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H11Br2NO2/c1-10-7-8-12-13(18)9-14(19)16(15(12)20-10)22-17(21)11-5-3-2-4-6-11/h2-9H,1H3
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| Chemical Name |
5,7-Dibromo-2-methyl-8-quinolinol benzoate ester
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| Synonyms |
Broxaldine; AL 307; AL-307; AL307
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| HS Tariff Code |
2934.99.03.00
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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) |
DMSO : 8.33 ~30 mg/mL ( 19.78 ~71.24 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.97 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.83 mg/mL (1.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 8.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10% DMSO+90% Corn Oil: ≥ 0.83 mg/mL (1.97 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3748 mL | 11.8742 mL | 23.7485 mL | |
| 5 mM | 0.4750 mL | 2.3748 mL | 4.7497 mL | |
| 10 mM | 0.2375 mL | 1.1874 mL | 2.3748 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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