Rifaximin (Xifaxan)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Rifaximin是利福霉素衍生物,是一种不可吸收的抗生素。Rifaximin通过结合细菌DNA依赖性的RNA聚合酶的β亚基来抑制RNA合成。
体外实验:Rifaximin是人类核受体孕烷-X受体(PXR)的肠特异性配体,有助于维持肠免疫稳态。Rifaximin消除了LPS引起的NF-κB的结合。在来自炎症性肠病患者的人结肠活检中,Rifaximin(100 μM)降低了由LPS刺激诱导的IL-8、Rantes、MIP-3α和TNFα的mRNA水平[1]。Rifaximin作用于细菌的脱氧核糖核酸(DNA)-依赖性核糖核酸(RNA)聚合酶的β亚基以抑制细菌RNA合成。革兰氏阳性菌对Rifaximin的敏感性大于革兰氏阴性菌[2]。在转染稳定表达重组人PXR的DPX2细胞系中, Rifaximin浓度大于1 μM时hPXR显著活化,EC50约为20 μM[3]。
在体实验:在用Rifaximin治疗的hPXR小鼠的小肠中,几种PXR靶基因例如CYP3A11、GSTA1、MRP2和OATP2的表达上调。在野生型、Pxr无效和hPXR小鼠中,Rifaximin对肝PXR靶基因没有显著影响[3]。在PXR人源化小鼠中,长期给予rifaximin 6个月可上调与甘油三酯合成和脂质积累相关的肝脏基因的表达[4]。
临床试验:在6个月的时间里,Rifaximin治疗有效地缓解了肝性脑病。Rifaximin显著降低涉及肝性脑病的住院风险[5]。在肠易激综合征(IBS)而不便秘的患者中,Rifaximin治疗2周可显著缓解IBS症状、腹胀、腹部疼痛和松散或水样的粪便[6]。Rifaximin可以改善IBS患者的症状,如腹胀和胃肠胀气[7]。
参考文献:
Mencarelli A, Renga B, Palladino G, et al. Inhibition of NF-κB by a PXR-dependent pathway mediates counter-regulatory activities of rifaximin on innate immunity in intestinal epithelial cells[J]. European journal of pharmacology, 2011, 668(1): 317-324.
Gillis J C, Brogden R N. Rifaximin[J]. Drugs, 1995, 49(3): 467-484.
Ma X, Shah Y M, Guo G L, et al. Rifaximin is a gut-specific human pregnane X receptor activator[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 322(1): 391-398.
Cheng J, Krausz K, Tanaka N, et al. Chronic exposure to rifaximin causes hepatic steatosis in pregnane X receptor-humanized mice[J]. Toxicological Sciences, 2012: kfs211.
Bass N M, Mullen K D, Sanyal A, et al. Rifaximin treatment in hepatic encephalopathy[J]. New England Journal of Medicine, 2010, 362(12): 1071-1081.
Pimentel M, Lembo A, Chey W D, et al. Rifaximin therapy for patients with irritable bowel syndrome without constipation[J]. New england journal of medicine, 2011, 364(1): 22-32.
Sharara A I, Aoun E, Abdul-Baki H, et al. A randomized double-blind placebo-controlled trial of rifaximin in patients with abdominal bloating and flatulence[J]. The American journal of gastroenterology, 2006, 101(2): 326-333.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 785.88 |
Cas No. | 80621-81-4 |
Formula | C43H51N3O11 |
Solubility | ≥83.33 mg/mL in DMSO; insoluble in H2O; ≥30 mg/mL in EtOH with ultrasonic |
SDF | Download SDF |
Canonical SMILES | O[C@@H]([C@H](C)[C@H]([C@H](/C=C/C=C(C)\C(NC1=C2O)=O)C)O)[C@@H](C)[C@@H]([C@H](C)[C@H](/C=C/O[C@@](C3=O)(C)OC4=C3C(C5=C1N(C=CC(C)=C6)C6=N5)=C2C(O)=C4C)OC)OC(C)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
CRL1831细胞 |
制备方法 |
在DMSO中的溶解度大于39.3mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
50 μM;3小时 |
实验结果 |
Rifaximin抑制LPS诱导的NF-κB DNA结合活性,从而下调细胞因子与趋化因子的表达。此外,Rifaximin也增加经LPS诱导后PXR和NF-κB p65之间的物理结合程度。 |
动物实验 [2]: | |
动物模型 |
hPXR小鼠 |
给药剂量 |
1 mg/kg/day;口服给药;6个月 |
实验结果 |
在hPXR小鼠中,Rifaximin呈时间依赖性地逐渐改善肝细胞脂肪变性,同时,不会引起结节性增生。此外,与接受Rifaximin治疗1周的hPXR小鼠相比,接受Rifaximin治疗1个月、3个月和6个月的hPXR小鼠的血清甘油三酯和血清游离脂肪酸显著降低。然而,接受Rifaximin治疗1周、1个月、3个月和6个月的hPXR小鼠的血清ALT和AST活性无显著差异。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Mencarelli A, Renga B, Palladino G, et al. Inhibition of NF-κB by a PXR-dependent pathway mediates counter-regulatory activities of rifaximin on innate immunity in intestinal epithelial cells[J]. European journal of pharmacology, 2011, 668(1): 317-324. [2]. Cheng J, Krausz K, Tanaka N, et al. Chronic exposure to rifaximin causes hepatic steatosis in pregnane X receptor-humanized mice[J]. Toxicological Sciences, 2012: kfs211 |
质量控制和MSDS
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