BTZ043 Racemate
(Synonyms: BTZ10526038; Benzothiazinone 10526038) 目录号 : GC18127
BTZ043外消旋体（BTZ10526038）是BTZ043的外消旋体。
Cas No.:957217-65-1
Sample solution is provided at 25 µL, 10mM.
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MIC: 1 ng/ml (2.3 nM) for M. tuberculosis H37Rv and 4 ng/ml (9.2 nM) for Mycobacterium smegmatis
The loss of human lives to tuberculosis (TB) continues unabated as a result of poverty, synergy with the HIV/AIDS pandemic, and the emergence of multidrug- and extensively drug-resistant strains of Mycobacterium tuberculosis. BTZ043 is the most advanced candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant TB.
In vitro: BTZ043 displayed similar activity against all clinical isolates of M. tuberculosis that were tested, including extensively drug-resistant and multidrug-resistant strains, indicating that it targets a previously unknown biological function. BTZ043 is bactericidal, reducing viability in vitro by more than 1000-fold in under 72 hours, which is comparable to the INH killing effect [1].
In vivo: The in vivo efficacy of BTZ043 was assessed 4 weeks after a low-dose aerosol infection of in the chronic BALB/c mice model of TB. Four weeks of treatment with BTZ043 reduced the bacterial load in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. Additional findings suggest that BTZ efficacy is time- rather than dose-dependent [1].
Clinical trial: Up to now, BTZ043 is still in the preclinical development stage.
Reference:
[1] Makarov V, Manina G, Mikusova K, et al. Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. Science. 2009 May 8;324(5928):801-4.
| Cas No. | 957217-65-1 | SDF | |
| 别名 | BTZ10526038; Benzothiazinone 10526038 | ||
| 化学名 | 2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one | ||
| Canonical SMILES | CC1COC2(O1)CCN(CC2)C3=NC(=O)C4=CC(=CC(=C4S3)[N+](=O)[O-])C(F)(F)F | ||
| 分子式 | C17H16F3N3O5S | 分子量 | 431.39 |
| 溶解度 | ≥ 10.4mg/mL in DMSO with gentle warming, ≥ 3.27 mg/mL in EtOH with ultrasonic and warming | 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 | 2.3181 mL | 11.5904 mL | 23.1809 mL |
| 5 mM | 0.4636 mL | 2.3181 mL | 4.6362 mL |
| 10 mM | 0.2318 mL | 1.159 mL | 2.3181 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet