Rifampin (NSC-113926)

Catalog No.S1764 Synonyms: Rimactane, Rifampicin

For research use only.

Rifampin (NSC-113926, Rimactane, Rifampicin) is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.

Rifampin (NSC-113926) Chemical Structure

CAS No. 13292-46-1

Selleck's Rifampin (NSC-113926) has been cited by 9 Publications

Purity & Quality Control

Choose Selective Antineoplastic and Immunosuppressive Antibiotics Inhibitors

Biological Activity

Description Rifampin (NSC-113926, Rimactane, Rifampicin) is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.
Targets
RNA polymerase [1]
In vitro

Rifampin inhibits IκBα degradation and mitogen-activated protein kinase (MAPK) phosphorylation. Rifampin is found to bind to human MD-2 in a Rifampin and MD-2 concentration-dependent manner. Rifampin inhibits NF-κB activation induced by LPS (20 ng/ml) in a dose-dependent manner, with an IC50 of 44.1 μM in Blue hTLR4 293 cells (A) and immunocompetent microgial BV-2 cell. Rifampin (50 μM) suppresses NF-κB activation at varying LPS doses, and the maximum NF-κB level induced by LPS in the presence of Rifampin (50 μM) is much lower than that in the absence of Rifampin. Rifampin inhibits NO production induced by LPS (200 ng/ml) in a dose-dependent manner in BV-2 cells, with an IC50 of 21.2 μM. Rifampin suppresses LPS induced TNF-α and IL-1β production in both microglia BV-2 and RAW 264.7 macrophage cells. Rifampin-inhibiting innate immune signaling is independent of the pregnane X receptor NR1I2. [1] Rifampin combined with polyester vascular prostheses (PVP) functionalised with cyclodextrin (PVP-CD) results in significant bacterial adhesion reduction and growth inhibition against Gram-positive bacteria. [2] Rifampin (50 μg/mL) significantly reduces the CFU counts of stationary-phase cultures and reduces the CFU counts of the log-phase culture to zero. Rifampin is particularly suitable since it is bactericidal and starts killing M. tuberculosis within an hour of exposure. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(121.51 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 822.94
Formula

C43H58N4O12

CAS No. 13292-46-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1C=CC=C(C(=O)NC2=C(C(=C3C(=C2O)C(=C(C4=C3C(=O)C(O4)(OC=CC(C(C(C(C(C(C1O)C)O)C)OC(=O)C)C)OC)C)C)O)O)C=NN5CCN(CC5)C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04933682 Completed Drug: ALXN2050|Drug: Fluconazole|Drug: Rifampin Healthy Alexion Pharmaceuticals June 23 2021 Phase 1
NCT04775238 Recruiting Other: Silver nanoparticles|Other: Copper nanoparticles Nosocomial Infections Sohag University February 27 2021 Not Applicable
NCT04301310 Not yet recruiting Drug: BMS-986235 (Treatment A)|Drug: Rifampin (Treatment B) Healthy Participants Bristol-Myers Squibb May 15 2020 Phase 1
NCT04537715 Recruiting Drug: Tazemetostat|Drug: Itraconazole|Drug: Rifampin All Malignancies|Advanced Malignancies|Hematologic Malignancy|Solid Tumor|Follicular Lymphoma (FL)|Non-Hodgkin Lymphoma (NHL)|Diffuse Large B-Cell Lymphoma (DLBCL)|Epithelioid Sarcoma (ES)|Synovial Sarcoma|Renal Medullary Carcinoma|Mesothelioma|Rhabdoid Tumor Epizyme Inc. April 23 2020 Phase 1
NCT04312282 Terminated Drug: Tesetaxel|Drug: Itraconazole|Drug: Rifampin Advanced Solid Tumors Odonate Therapeutics Inc. March 6 2020 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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