research use only
Cat.No.S1790
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Other DNA/RNA Synthesis Inhibitors | CX-5461 (Pidnarulex) B02 SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Triapine (3-AP) Carmofur YK-4-279 |
|
In vitro |
Ethanol : 157 mg/mL
DMSO
: 47 mg/mL
(59.8 mM)
Water : Insoluble |
|
In vivo |
|||||
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Molecular Weight | 785.88 | Formula | C43H51N3O11 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 80621-81-4 | Download SDF | Storage of Stock Solutions |
|
|
| Synonyms | N/A | Smiles | CC1C=CC=C(C(=O)NC2=C(C3=C(C4=C(C(=C3O)C)OC(C4=O)(OC=CC(C(C(C(C(C(C1O)C)O)C)OC(=O)C)C)OC)C)C5=C2N6C=CC(=CC6=N5)C)O)C | ||
| Targets/IC50/Ki |
RNA polymerase
|
|---|---|
| In vitro |
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. This compound inhibits the LPS-induced cytokine and chemokine expression by suppressing NF-κB DNA-binding activity. It (100 μM) effectively decreases the expression of TNFα, IL-8, MIP-3α and Rantes induced by LPS stimulation (100 μg/mL). This chemical binds the β subunit of the bacterial DNA-dependent RNA polymerase, inhibiting the initiation of chain formation in RNA synthesis. It has a lower MIC against gram-positive bacteria, with an MIC90 at dosages ranging from 0.01 µg/mL to 0.5 µg/mL. This agent has broad-spectrum activity against aerobic and anaerobic gram-positive and gram-negative microorganisms. |
| In vivo |
Rifaximin is highly concentrated in the intestinal tract compared with rifampicin. This compound treatment results in significant induction of PXR target genes in the intestine of hPXR mice, but not in wild-type and Pxr-null mice. This chemical-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. It 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. |
References |
|
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05408910 | Not yet recruiting | Cystic Fibrosis|Abdominal Pain|Small Bowel Disease |
Wake Forest University Health Sciences|Nationwide Children''s Hospital|University of Minnesota|University of Texas Southwestern Medical Center |
July 2024 | Phase 2|Phase 3 |
| NCT06298409 | Recruiting | Small Intestinal Bacterial Overgrowth |
Envivo Bio Inc |
February 15 2024 | -- |
| NCT04244877 | Withdrawn | Cirrhosis Liver|Minimal Hepatic Encephalopathy|Small Intestinal Bacterial Overgrowth|Gastrointestinal Motility Disorder |
MetroHealth Medical Center |
September 15 2021 | Phase 3 |
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.