Rifaximin
目录号 : KM8906 CAS No. : 80621-81-4 纯度 : 98%

Rifaximin是一种胃肠道选择性的抗生素 (antibiotic),与细菌 DNA 依赖性 RNA 聚合酶的 β 亚基结合,从而抑制细菌 RNA 的合成 (bacterial RNA synthesis)。与革兰氏阴性菌(MIC:8-50 毫克/毫升)相比,Rifaximin对革兰氏阳性菌株(MIC:0.03-5 毫克/毫升)的敏感性更高。

规格 价格 是否有货 数量
500mg
In-stock
1g
In-stock
5g
In-stock
10g 询价 In-stock
50g 询价 In-stock

Other Forms of Rapamycin:

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生物活性

Rifaximin, a gastrointestinal-selective antibiotic, binds the β-subunit of bacterial DNA-dependent RNA polymerase, resulting in inhibition of bacterial RNA synthesis. Rifaximin susceptibility is higher against Gram-positive strains (MIC: 0.03-5 mg/ml) compared to Gram-negative bacteria (MIC: 8-50 mg/mL).

体外研究

Rifaximin has a good inhibitory activity against Staphylococcus, Streptococcus, Enterococcus, Escherichia coli, Shigella, Salmonella, Bacillus cereus, Moraxella catarrhalis, Haemophilus influenzae, Haemophilus ducreyi, Bacteroides bivius-disiens, Gardnerella vaginalis, Lactobacillus spp.,Mobiluncus spp.,Neisseria gonorrhoeae, Pseudomonas and Acinetobacter . Rifaximin rarely causes side effects.
Rifaximin (0.1, 1.0 and 10.0 µM) causes significant and concentration-dependent reduction of cell proliferation, cell migration and PCNA expression in the Caco-2 cells vs. untreated cells.
Rifaximin (0.1-10 μM) downregulates Akt/mTOR and p38MAPK/NF-κB pathways through a PXR-dependent mechanism.

Cell Viability Assay

Cell Line: Caco-2 cells
Concentration: 0.1, 1.0 and 10.0 μM
Incubation Time: 48 hours
Result: Caused a significant and concentration-dependent reduction in cell proliferation. Reduced the expression of PCNA in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Caco-2 cells
Concentration: 0.1, 1.0 and 10.0 μM
Incubation Time: 24 hours
Result: Reduced Akt, mTOR, p38 MAPK and HIF-1α expression in a concentration-dependent manner. Inhibited NF-κB nuclear activation and p70S6K.
体内研究

Rifaximin administration (30 or 50 mg/kg/day) increases survival rates of colitic mice and reduces colitis severity by improvement of wasting syndrome, histologic scores, decrease in colon IL-2, IL-12, IFN-gamma and TNF-alpha (protein and mRNA) levels, and diminishes colon myeloperoxidase (MPO) activity.

Animal Model: Balb/c mice (6–8 weeks old) bearing 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis
Dosage: 10, 30 and 50 mg/kg/day
Administration: Orally, p.o. daily for 7 days
Result: Significantly reduced TNBS induced colitis at the dose of 30 and 50 mg/kg, but not 10 mg/kg. A 7-day course of 30 and 50 mg/kg resulted in an almost complete tissue protection.
分子式
C43H51N3O11
分子量
785.88
CAS号
80621-81-4
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (63.62 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 1.2725 mL 6.3623 mL 12.7246 mL
5 mM 0.2545 mL 1.2725 mL 2.5449 mL
10 mM 0.1272 mL 0.6362 mL 1.2725 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;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, 6 months; -20°C, 1 month。-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。

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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (3.82 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (3.82 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 30.0 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (3.82 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (3.82 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 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.65 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (2.65 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

临床试验
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