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Eravacycline dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Eravacycline dihydrochloride图片
CAS NO:1334714-66-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
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-spectrumantibacterialagent.

体外研究
(In Vitro)

Eravacycline is potent antibiotic againstA. 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 MIC50/90values are 0.5/1 mg/L[1]. Eravacycline shows inhibitory effects on six E. coli with MICs ranging from 0.125 to 0.25 mg/L[2]. 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 exceptP. aeruginosa, as well as excellent activity against major gram-positive pathogens, including methicillin-resistantS. aureus. Eravacycline also displays potent ribosomal inhibition[3]. 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 ofPseudomonas aeruginosaandBurkholderia 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].

体内研究
(In Vivo)

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[2]. 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.) againstStaphylococcus aureus. The PD50values againstEscherichia coliisolates are 1.2 to 4.4 mg/kg q.d[5].

Clinical Trial
分子量

631.48

性状

Solid

Formula

C27H33Cl2FN4O8

CAS 号

1334714-66-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-80°C, protect from light, stored under nitrogen

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

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 mg5 mg10 mg
1 mM1.5836 mL7.9179 mL15.8358 mL
5 mM0.3167 mL1.5836 mL3.1672 mL
10 mM0.1584 mL0.7918 mL1.5836 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-CDin 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 μL20% 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。

*以上所有助溶剂都可在本网站选购。