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  1. Anti-infection Cell Cycle/DNA Damage
  2. Bacterial Antibiotic DNA/RNA Synthesis
  3. Rifaximin

Rifaximin是一種胃腸道選擇性的抗生素 (antibiotic),與細(xì)菌 DNA 依賴性 RNA 聚合酶的 β 亞基結(jié)合,從而抑制細(xì)菌 RNA 的合成 (bacterial RNA synthesis)。與革蘭氏陰性菌(MIC:8-50 毫克/毫升)相比,Rifaximin對(duì)革蘭氏陽(yáng)性菌株(MIC:0.03-5 毫克/毫升)的敏感性更高。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Rifaximin Chemical Structure

Rifaximin Chemical Structure

CAS No. : 80621-81-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥572
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500 mg ¥520
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1 g ¥836
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5 g ¥3100
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Customer Review

Other Forms of Rifaximin:

MCE 顧客使用本產(chǎn)品發(fā)表的 3 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)[1][2].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 EC50
11.2 μM
Compound: Rifaximin
Transactivation of full length human PXR transfected in human HepG2 cells after 18 hrs by luciferase reporter assay relative to rifaximin
Transactivation of full length human PXR transfected in human HepG2 cells after 18 hrs by luciferase reporter assay relative to rifaximin
[PMID: 26408814]
HepG2 EC50
14.1 μM
Compound: Rifaximin
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
[PMID: 20966043]
HepG2 EC50
14.1 μM
Compound: Rifaximin
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
HepG2 EC50
2.2 μM
Compound: rifaximin
Transactivation of human PXR expressed in HepG2 cells after 18 hrs by luciferase reporter gene assay
Transactivation of human PXR expressed in HepG2 cells after 18 hrs by luciferase reporter gene assay
[PMID: 21599020]
HepG2 EC50
4 μM
Compound: rifaximin
Agonist activity at human full-length PXR transfected in human HepG2 cells co-transfected with pSG5-RXR assessed as induction of transactivation by dual-luciferase reporter gene assay
Agonist activity at human full-length PXR transfected in human HepG2 cells co-transfected with pSG5-RXR assessed as induction of transactivation by dual-luciferase reporter gene assay
[PMID: 24388834]
體外研究
(In Vitro)

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[1].
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[2].
Rifaximin (0.1-10 μM) downregulates Akt/mTOR and p38MAPK/NF-κB pathways through a PXR-dependent mechanism[2].

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

Cell Viability Assay[2]

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[2]

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.
體內(nèi)研究
(In Vivo)

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[3].

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

Animal Model: Balb/c mice (6–8 weeks old) bearing 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis[3]
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.
Clinical Trial
分子量

785.88

Formula

C43H51N3O11

CAS 號(hào)
性狀

固體

顏色

Yellow to orange

中文名稱

利福昔明

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : ≥ 50 mg/mL (63.62 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3 mg/mL (3.82 mM); 澄清溶液

    此方案可獲得 ≥ 3 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 30.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

    Solubility: ≥ 3 mg/mL (3.82 mM); 澄清溶液

    此方案可獲得 ≥ 3 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    1 mL 工作液為例,取 100 μL 30.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購(gòu)。 Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.88%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2725 mL 6.3623 mL 12.7246 mL 31.8115 mL
5 mM 0.2545 mL 1.2725 mL 2.5449 mL 6.3623 mL
10 mM 0.1272 mL 0.6362 mL 1.2725 mL 3.1811 mL
15 mM 0.0848 mL 0.4242 mL 0.8483 mL 2.1208 mL
20 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5906 mL
25 mM 0.0509 mL 0.2545 mL 0.5090 mL 1.2725 mL
30 mM 0.0424 mL 0.2121 mL 0.4242 mL 1.0604 mL
40 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.7953 mL
50 mM 0.0254 mL 0.1272 mL 0.2545 mL 0.6362 mL
60 mM 0.0212 mL 0.1060 mL 0.2121 mL 0.5302 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱:
Rifaximin
目錄號(hào):
HY-13234
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