Eravacycline dihydrochloride TP-434 dihydrochloride; TP-434-046|cas:1334714-66-7|西域试剂

Eravacycline dihydrochloride TP-434 dihydrochloride; TP-434-046,98.98%

产品编号：Bellancom-16980A| CAS NO：1334714-66-7| 分子式：C₂₇H₃₃Cl₂FN₄O₈| 分子量：631.48

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货号	价格	库存与货期
Bellancom-16980A	￥2400.00	杭州北京（现货）
Bellancom-16980A	￥8500.00	杭州北京（现货）
Bellancom-16980A	￥10500.00	杭州北京（现货）

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Eravacycline dihydrochloride TP-434 dihydrochloride; TP-434-046

产品介绍

Eravacycline dihydrochloride (TP-434 dihydrochloride) 是一种有效的广谱抗菌剂。

生物活性

Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.

体外研究

Eravacycline is potent antibiotic against A. baumannii, including isolates that are resistant to sulbactam, SM 7338, and BAY 41-6551. Eravacycline shows greater activity than BAY 41-6551, and colistin. The eravacycline MIC₅₀/₉₀ values are 0.5/1 mg/L. Eravacycline shows inhibitory effects on six E. coli with MICs ranging from 0.125 to 0.25 mg/L. Eravacycline dihydrochloride is a synthetic antibiotic, with inhibits bacterial protein synthesis through binding to the 30S ribosomal subunit. Eravacycline displays broad spectrum activity against gram-negative bacteria in the panel except P. aeruginosa, as well as excellent activity against major gram-positive pathogens, including methicillin-resistant S. aureus. Eravacycline also displays potent ribosomal inhibition. Eravacycline shows potent broad-spectrum activity against 90% of the isolates (MIC₉₀) in each panel at concentrations ranging from ≤0.008 to 2 μg/mL for all species panels except those of Pseudomonas aeruginosa and Burkholderia cenocepacia ((MIC₉₀) values of 32 μg/mL for both organisms). Eravacycline is active against multidrug-resistant bacteria, including those expressing extended-spectrum β-lactamases and mechanisms conferring resistance to other classes of antibiotics, including carbapenem resistance^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Mice are treated with two-fold increasing doses (range 3.125 to 50 mg/kg) of eravacycline every 12 hours. The mean fAUC/MIC magnitude associated with net stasis and 1-log kill endpoint are 27.97 ± 8.29 and 32.60 ± 10.85, respectively. Eravacycline is active in multiple murine models of infection against clinically important Gram-positive and Gram-negative pathogens. Eravacycline is efficacious in mouse septicemia models, demonstrating 50% protective dose values of ≤1 mg/kg of body weight once a day (q.d.) against Staphylococcus aureus. The PD₅₀ values against Escherichia coli isolates are 1.2 to 4.4 mg/kg q.d^[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

H₂O : 50 mg/mL (79.18 mM; Need ultrasonic)

DMSO : ≥ 50 mg/mL (79.18 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5836 mL	7.9179 mL	15.8358 mL
5 mM	0.3167 mL	1.5836 mL	3.1672 mL
10 mM	0.1584 mL	0.7918 mL	1.5836 mL

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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (79.18 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5.5 mg/mL (8.71 mM); Clear solution

此方案可获得 ≥ 5.5 mg/mL (8.71 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5.5 mg/mL (8.71 mM); Clear solution

此方案可获得 ≥ 5.5 mg/mL (8.71 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5.5 mg/mL (8.71 mM); Clear solution

此方案可获得 ≥ 5.5 mg/mL (8.71 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。