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Rifaximin
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。
Rifaximin图片
CAS NO:80621-81-4
规格:≥98%
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)785.88
FormulaC43H51N3O11
CAS No.80621-81-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 47 mg/mL (59.8 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (3.8 mM)
Other info

Chemical Name: (2S,18E,28E)-25S-(acetyloxy)-5,6,21S,23R-tetrahydroxy-27S-methoxy-2,4,11,16Z,20S,22R,24R,26R-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione

InChi Key: NZCRJKRKKOLAOJ-XRCRFVBUSA-N

InChi Code: InChI=1S/C43H51N3O11/c1-19-14-16-46-28(18-19)44-32-29-30-37(50)25(7)40-31(29)41(52)43(9,57-40)55-17-15-27(54-10)22(4)39(56-26(8)47)24(6)36(49)23(5)35(48)20(2)12-11-13-21(3)42(53)45-33(34(32)46)38(30)51/h11-18,20,22-24,27,35-36,39,48-51H,1-10H3,(H,45,53)/b12-11+,17-15+,21-13-/t20-,22+,23+,24+,27-,35-,36+,39+,43-/m0/s1

SMILES Code: OC1=C(NC(/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@H](C)[C@@H](OC)/C=C/O[C@@](C2=O)(C)O3)=O)C4=C(N=C5N4C=CC(C)=C5)C6=C2C3=C(C)C(O)=C61

Synonyms

BRN-3584528; L-105; BRN 3584528; L105; BRN3584528; L 105SV; Fatroximin; Normix; Rifacol; Rifamycin L 105; Rifaxidin; Rifaximin; Rifaxin; Ritacol; Rifaximin; trade names: RCIFAX, Rifagut, Xifaxan, Zaxine

实验参考方法
In Vitro

In vitro activity: Rifaximin (50 μM) reduces changes in the production of proinflammatory factors caused by LPS stimulation in IEC, such as TNF-α, IL-8, Rantes and PGE2 in normal intestinal epithelial cells. Rifaximin inhibits the LPS-induced cytokine and chemokine expression by suppressing NF-κB DNA-binding activity. Rifaximin (100 μM) effectively decreases the expression of TNFα, IL-8, MIP-3α and Rantes induced by LPS stimulation (100 μg/mL). Rifaximin binds the β subunit of the bacterial DNA-dependent RNA polymerase, inhibiting the initiation of chain formation in RNA synthesis. Rifaximin has a lower MIC against gram-positive bacteria, with an MIC90 at dosages ranging from 0.01 μg/mL to 0.5 μg/mL. Rifaximin has broad-spectrum activity against aerobic and anaerobic gram-positive and gram-negative microorganisms.

In VivoRifaximin is highly concentrated in the intestinal tract compared with rifampicin. Rifaximin treatment results in significant induction of PXR target genes in the intestine of hPXR mice, but not in wild-type and Pxr-null mice. Rifaximin-mediated activation of human PXR, but not the other xenobiotic nuclear receptors constitutive androstane receptor, peroxisome proliferator-activated receptor (PPAR)alpha, PPARgamma, and farnesoid X receptor. Rifaximin could lead to PXR-dependent hepatocellular fatty degeneration as a result of activation of genes involved in lipid uptake, thus indicating a potential adverse effect of rifaximin on liver function after long-term exposure.
Animal modelMice
Formulation & DosageN/A
References

Eur J Pharmacol. 2011 Oct 1;668(1-2):317-24; J Pharmacol Exp Ther. 2007 Jul;322(1):391-8.