BRD-8000.3是一种特异性EfpA抑制剂，是一种窄谱杀菌抗真菌剂，具有良好的野生型活性。
Cas No.:2365504-95-4
Sample solution is provided at 25 µL, 10mM.
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BRD-8000.3, as a specific EfpA inhibitor, is a narrow-spectrum, bactericidal antimycobacterial agent with good wild-type activity[1]. BRD-8000.3 exhibits inhibitory activity against Mycobacterium tuberculosis (Mtb) with an MIC₉₀ value of 800nM[1]. Resistance to BRD-8000.3 could be conferred by mutations in EfpA, including substitutions V319F and A415V[2].
In vitro, BRD-8000.3 has an IC50 value greater than 50μM for HepG2[3].
In vivo, BRD-8000.3, administered orally at 150mg/kg, demonstrated good mouse plasma exposure and low risk for drug–drug interactions, prolongation of the QT interval, or hepatotoxicity[3].
References:
[1] Johnson EO, et al. Large-Scale Chemical-Genetic Strategy Enables the Design of Antimicrobial Combination Chemotherapy in Mycobacteria. ACS Infect Dis. 2020;6(1):56-63.
[2] Khandelwal NK, Gupta M, Gomez JE, et al. Structure and inhibition mechanisms of Mycobacterium tuberculosis essential transporter efflux protein A. Preprint. bioRxiv. 2024;2024.09.04.611325.
[3] Johnson EO, LaVerriere E, Office E, et al. Large-scale chemical-genetics yields new M. tuberculosis inhibitor classes. Nature. 2019;571(7763):72-78.
BRD-8000.3是一种特异性EfpA抑制剂，是一种窄谱杀菌抗真菌剂，具有良好的野生型活性[1]。BRD-8000.3对结核分枝杆菌（Mtb）具有抑制活性，MIC₉₀值为800nM[1]。BRD-8000.3的耐药性可以通过EfpA突变获得，包括V319F和A415V的替换[2]。
体外实验中，BRD-8000.3对HepG2细胞的IC50值大于50μM[3]。
体内实验中，以150mg/kg的剂量口服给药的BRD-8000.3表现出良好的小鼠血浆暴露水平，且药物之间的相互作用风险、QT间期延长风险或肝毒性风险均较低[3]。
| Animal experiment [1]: | |
Animal models | C57BL/6 mice |
Preparation Method | Oral dosing of 12h fasted female 7-9-week-old C57BL/6 mice was performed, using 150mg/kg BRD-8000.3 in 5% (v/v) corn oil, 10% (v/v) labrasol, 5% (v/v) solutol in water. The plasma concentration of BRD-8000.3 was measured at nine time points up to 8h. |
Dosage form | 150mg/kg; p.o. |
Applications | BRD-8000.3 showed good mouse plasma exposure by oral dosing. The half-life of BRD-8000.3 in mice is 5min. |
References: | |
| Cas No. | 2365504-95-4 | SDF | |
| 分子式 | C19H21BrN4O | 分子量 | 401.3 |
| 溶解度 | DMSO : 50 mg/mL (124.60 mM; Need ultrasonic) | 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 | 2.4919 mL | 12.4595 mL | 24.919 mL |
| 5 mM | 498.4 μL | 2.4919 mL | 4.9838 mL |
| 10 mM | 249.2 μL | 1.246 mL | 2.4919 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet