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TCA1

产品编号 T5315 CAS 864941-32-2

别名: TCA-1, TCA 1

TCA1 (TCA 1) 是一种小分子，具有抗耐药性和持续性结核病的活性。

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TCA1, CAS 864941-32-2

规格	价格/CNY	货期
1 mg	￥ 459	现货
2 mg	￥ 666	现货
5 mg	￥ 997	现货
10 mg	￥ 1,530	现货
25 mg	￥ 2,860	现货
50 mg	￥ 4,230	现货
100 mg	￥ 5,930	现货
1 mL * 10 mM (in DMSO)	￥ 997	现货

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纯度: 97.23%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	TCA1 (TCA 1) is a small molecule with activity against drug-resistant and persistent tuberculosis.
体外活性	The activities of TCA1 against M. smegmatis, M. bovis bacillus Calmette–Guérin, and Mtb are 20- to 150-fold higher in biofilm medium (MIC50 = 0.03, 0.04, and 0.01 μg/mL, respectively) than 7H9 medium (MIC50 = 4.5, 3, and 0.19 μg/mL, respectively). TCA1 is bactericidal with an MIC99 value of 2.1 μg/mL in solid medium.
体内活性	After i.v. administration, TCA1 exhibited a low clearance and steady-state volume of distribution, with an elimination half-life of 0.73 h. After oral administration of 20 and 50 mg/kg in solution formulation, TCA1 showed a high Cmax (2,122 and 5,653 nM, respectively), moderate exposure with oral bioavailability ranging from 19% to 46%, and a half-life of 1.8 h. BALB/c mice were infected with a low dose of Mtb H37Rv (～200 bacilli); 2 wk after infection, mice were treated with TCA1 (40 mg/kg) for 4 wk (dosed 1 time/d for 5 d/wk). After 4 wk of treatment with TCA1, the cfu dropped 0.5 log in lung and 1.5 logs in spleen.
细胞实验	For kinetic killing assays, exponentially growing cultures of mycobacteria were diluted in fresh media to an OD600 of 0.1–0.2. Various drugs were added to the culture at the indicated concentrations. The number of cfus at the start of the experiment was estimated by plating appropriate dilutions of the culture onto 7H10 agar plates. The effect of drug was monitored by plating for cfus at the indicated time points. All experiments were carried out in triplicate. MICs were determined by a turbidity assay. Threefold serial dilutions in DMSO were prepared for each compound. Mtb cultures (OD = 0.04) were incubated with compounds at 37 °C for 5 d, and OD600 was determined with an Envision plate reader. All experiments were carried out in duplicate. For assays under starvation conditions, a log-phase growing Mtb culture was centrifuged, and the cell pellet was washed two times with PBS, resuspended in PBS with Tyloxapol (0.05%; OD = 0.3), and incubated with DMSO, TCA1 (7.5 μg/mL), and RIF (2 μg/mL). All experiments were carried out in triplicate. For intracellular macrophage assays, J744.1 murine macrophage cells were infected with Mtb at a multiplicity of infection (MOI) of 1:3 and incubated for 2 h at 37 °C. After washing the cell monolayer three times, 20 μM amikacin was added, and the culture was incubated for an additional 2 h to kill the remaining extracellular bacteria. Infected cells were then incubated in the presence of serial dilutions of compounds for 5 d. Cells were washed three times and lysed in each well; the lysate was transferred to a 96-well plate for serial dilution and then plated on 7H11 agar medium for cfu assays.
动物实验	Six- to eight-week-old female BALB/c mice were infected by aerosol with a low dose (～50 bacilli) of Mtb H37Rv. Infection dose was verified by plating the inoculum and the whole-lung homogenates onto 7H10 plates at 24 h postinfection. Treatment of BALB/c mice began at either 2 or 4 wk postinfection, with RIF (10 mg/kg) and INH (25 mg/kg) administered ad libitum in drinking water (changed one time every 2 d). TCA1 was administered by oral gavage one time daily for 5 d/wk at a dosage of either 40 or 100 mg/kg for the indicated durations. At predetermined time points or humane endpoints, animals were heavily sedated and euthanized, and tissues were collected for culture and pathology. Treatment efficacy was assessed on the basis of cfu in the lungs and spleen of treated mice compared with untreated controls and bacterial burden in these organs before treatment start. Organs were homogenized in PBS containing Tween-80 [0.05% (vol/vol)], and various dilutions were placed on 7H10 plates. Plates were incubated at 37 °C for 3 wk, and cfus on the various plates were recorded.

别名	TCA-1, TCA 1
分子量	375.42
分子式	C16H13N3O4S2
CAS No.	864941-32-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 60 mg/mL (159.82 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6637 mL	13.3184 mL	26.6368 mL	66.5921 mL
	5 mM	0.5327 mL	2.6637 mL	5.3274 mL	13.3184 mL
	10 mM	0.2664 mL	1.3318 mL	2.6637 mL	6.6592 mL
	20 mM	0.1332 mL	0.6659 mL	1.3318 mL	3.3296 mL
	50 mM	0.0533 mL	0.2664 mL	0.5327 mL	1.3318 mL
	100 mM	0.0266 mL	0.1332 mL	0.2664 mL	0.6659 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Wang F, et al. Identification of a small molecule with activity against drug-resistant and persistent tuberculosis. Proc Natl Acad Sci U S A. 2013 Jul 2;110(27):E2510-7.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

TCA1 864941-32-2 Microbiology/Virology Antibacterial Antibiotic Inhibitor DprE1 Bacterial inhibit TCA-1 MoeW Mycobacterium tuberculosis TCA 1 oral inhibitor

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TCA1

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords