Retapamulin

Catalog No.S4056 Synonyms: SB-275833

For research use only.

Retapamulin (SB-275833) is a topical antibiotic, which binds to both E. coli and S. aureus ribosomes with similar potencies with Kd of 3 nM.

Retapamulin Chemical Structure

CAS No. 224452-66-8

Selleck's Retapamulin has been cited by 2 Publications

Purity & Quality Control

Choose Selective Antibiotics Inhibitors

Biological Activity

Description Retapamulin (SB-275833) is a topical antibiotic, which binds to both E. coli and S. aureus ribosomes with similar potencies with Kd of 3 nM.
Features Retapamulin is insoluble in water but is soluble in dimethyl sulfoxide and methanol.
Targets
ribosome [1] ribosome [1]
3 nM(Kd)
In vitro

Retapamulin is a potent inhibitor of protein synthesis with an IC50 of 0.33 μM in lysates prepared from erythromycin-susceptible E. coli cells. Retapamulin (100 μM) is ineffective in inhibiting eukaryotic translation when tested in a rabbit reticulocyte lysate system with the cellular components necessary for mammalian protein synthesis. Retapamulin binds to Erys ribosomes and fully displaces the labeled ligand with an IC50 of 26.1 nM. Retapamulin partially inhibits the ability of charged, N-blocked tRNA to bind to the P-site of E. coli ribosomes, with an IC50 of 17.4 nM (maximum inhibition of 80%). [1] Retapamulin inhibits Staphylococcus aureus and Streptococcus pyogenes with MIC90 of 0.12 μg/mL and ≤0.03 μg/mL, respectively. Retapamulin inhibits S. aureus subset with MIC50/90 values of 0.06/0.12 μg/mL. Retapamulin shows excellent activity against these isolates, with only two requiring a MIC of 0.06 μg/mL. [2] Retapamulin is very active against the S. pyogenes isolates tested with MIC90 of 0.016 μg/mL, and based on MIC90s, is 32- and >1,024-fold more active than mupirocin and fusidic acid, respectively. Retapamulin binds to a unique site on the bacterial ribosome, and by virtue of its novel mode of action. [3] Retapamulin (<2 mg/L) inhibits 37/52 (71%) strains of the B. fragilis group and 85/87 (98%) of the other Gram-negative bacilli. Retapamulin is more active than clindamycin, metronidazole and ceftriaxone against Propionibacterium acnes and anaerobic Gram-positive cocci. [4] Retapamulin inhibits total viable cells (TVC), Protein synthesis and 50S subunit synthesis in both wild-type (wt) Staphylococcus aureus strain RN1786 with IC50 of 12 ng/mL, 5 ng/mL and 27 ng/mL, respectively. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 517.76
Formula

C30H47NO4S

CAS No. 224452-66-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CCC23CCC(=O)C2C1(C(CC(C(C3C)O)(C)C=C)OC(=O)CSC4CC5CCC(C4)N5C)C

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03304873 Completed Drug: Retapamulin|Drug: Placebo Ointment MRSA NYU Langone Health December 1 2017 Phase 3
NCT01812382 Completed Drug: Retapamulin Microdialysis Skin Infections Bacterial GlaxoSmithKline April 2 2014 Phase 1
NCT01445600 Completed Drug: ALTARGO(retapamulin) Skin Infections Bacterial GlaxoSmithKline November 2012 --
NCT00903279 Withdrawn Drug: Placebo|Drug: Altabax (retapamulin) Orthopedic Procedures|Methicillin-resistant Staphylococcus Aureus Bay Pines VA Healthcare System August 2009 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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