Broxaldine (Brobenzoxaldine)
(Synonyms: 溴沙定; Brobenzoxaldine) 目录号 : GC32155
An antimicrobial agent
Cas No.:3684-46-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Broxaldine is an antimicrobial agent.1,2 It is active against the bacterium C. difficile (MIC = 4 ?M) and decreases the viability of S. mansoni larvae at 10 ?M.
1.AbdelKhalek, A., Mohammad, H., Mayhoub, A.S., et al.Screening for potent and selective anticlostridial leads among FDA-approved drugsJ. Antibiot. (Tokyo)73(6)392-409(2020) 2.Panic, G., Vargas, M., Scandale, I., et al.Activity profile of an FDA-approved compound library against Schistosoma mansoniPLoS Negl. Trop. Dis.9(7)e0003962(2015)
| Cas No. | 3684-46-6 | SDF | |
| 别名 | 溴沙定; Brobenzoxaldine | ||
| Canonical SMILES | CC1=NC2=C(OC(C3=CC=CC=C3)=O)C(Br)=CC(Br)=C2C=C1 | ||
| 分子式 | C17H11Br2NO2 | 分子量 | 421.08 |
| 溶解度 | DMSO : ≥ 42.86 mg/mL (101.79 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3748 mL | 11.8742 mL | 23.7485 mL |
| 5 mM | 0.475 mL | 2.3748 mL | 4.7497 mL |
| 10 mM | 0.2375 mL | 1.1874 mL | 2.3748 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Identification of Cytoprotective Small-Molecule Inducers of Heme-Oxygenase-1
Antioxidants (Basel) 2022 Sep 23;11(10):1888.PMID:36290611DOI:10.3390/antiox11101888.
Acute kidney injury (AKI) is a major public health concern with significant morbidity and mortality and no current treatments beyond supportive care and dialysis. Preclinical studies have suggested that heme-oxygenase-1 (HO-1), an enzyme that catalyzes the breakdown of heme, has promise as a potential therapeutic target for AKI. Clinical trials involving HO-1 products (biliverdin, carbon monoxide, and iron), however, have not progressed beyond the Phase ½ level. We identified small-molecule inducers of HO-1 that enable us to exploit the full therapeutic potential of HO-1, the combination of its products, and yet-undefined effects of the enzyme system. Through cell-based, high-throughput screens for induction of HO-1 driven by the human HO-1 promoter/enhancer, we identified two novel small molecules and Broxaldine (an FDA-approved drug) for further consideration as candidate compounds exhibiting an Emax ≿0% of 5 µM hemin and EC50 <10 µM. RNA sequencing identified shared binding motifs to NRF2, a transcription factor known to regulate antioxidant genes, including HMOX1. In vitro, the cytoprotective function of the candidates was assessed against cisplatin-induced cytotoxicity and apoptosis. In vivo, delivery of a candidate compound induced HO-1 expression in the kidneys of mice. This study serves as the basis for further development of small-molecule HO-1 inducers as preventative or therapeutic interventions for a variety of pathologies, including AKI.