化合物 TCA-1|T5315|TargetMol

價(jià)格	￥297	￥787	￥1230
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2025-05-20

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產(chǎn)品詳情

中文名稱:化合物 TCA-1	英文名稱:TCA1
CAS:864941-32-2	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
純度規(guī)格: 97.23%	產(chǎn)品類別: 抑制劑
貨號(hào): T5315

Product Introduction

Bioactivity

名稱	TCA1
描述	TCA1 (TCA 1) is a small molecule with activity against drug-resistant and persistent tuberculosis.
細(xì)胞實(shí)驗(yàn)	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.
動(dòng)物實(shí)驗(yàn)	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.
體外活性	TCA1對(duì)M. smegmatis、M. bovis bacillus Calmette–Guérin和Mtb的活性，在生物膜培養(yǎng)基中比在7H9培養(yǎng)基中高出20至150倍（分別為MIC50 = 0.03、0.04和0.01 μg/mL，相較于MIC50 = 4.5、3和0.19 μg/mL）。TCA1具有殺菌作用，在固體培養(yǎng)基中的MIC99值為2.1 μg/mL。
體內(nèi)活性	經(jīng)靜脈給藥后，TCA1顯示了低清除率和穩(wěn)定的分布體積，以及0.73小時(shí)的消除半衰期?？诜o予20和50 mg/kg溶液制劑后，TCA1表現(xiàn)出高Cmax（分別為2,122和5,653 nM），中等的暴露度，口服生物利用度在19%至46%之間，以及1.8小時(shí)的半衰期。BALB/c小鼠被低劑量的Mtb H37Rv（約200個(gè)菌落）感染；感染后2周，用TCA1（40 mg/kg）治療4周（每周5天，每天1次）。經(jīng)過(guò)4周的TCA1治療，肺中的cfu下降了0.5對(duì)數(shù)，脾臟中下降了1.5對(duì)數(shù)。
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 60 mg/mL (159.82 mM), Sonication is recommended.
關(guān)鍵字	tuberculosis \| TCA1 \| oral \| Mycobacterium \| MoeW \| Inhibitor \| inhibit \| DprE1 \| Bacterial
相關(guān)產(chǎn)品	Doxycycline (hyclate) \| Urethane \| Dehydroacetic acid sodium \| Doxycycline \| Methyl anthranilate \| Isoeugenol \| Neomycin sulfate \| Dimethyl sulfoxide \| EDTA copper(II) disodium salt \| Ampicillin sodium \| Sulfamethoxazole sodium \| Kanamycin sulfate
相關(guān)庫(kù)	經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 抗菌活性庫(kù) \| 抗生素庫(kù) \| 抗感染化合物庫(kù) \| NO PAINS 化合物庫(kù)

關(guān)鍵字： TCA-1|||TCA 1|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

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