Retapamulin

Catalog No.S4056 Synonyms: SB-275833

Retapamulin Chemical Structure

Molecular Weight(MW): 517.76

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

Size Price Stock Quantity  
In DMSO USD 350 In stock
USD 270 In stock
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Purity & Quality Control

Choose Selective Anti-infection Inhibitors

Biological Activity

Description Retapamulin 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

Solubility (25°C)

In vitro DMSO 104 mg/mL (200.86 mM)
Ethanol 104 mg/mL (200.86 mM)
Water 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 517.76
Formula

C30H47NO4S

CAS No. 224452-66-8
Storage powder
in solvent
Synonyms SB-275833

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03304873 Recruiting MRSA New York University School of Medicine December 1 2017 Phase 3
NCT03304873 Recruiting MRSA New York University School of Medicine December 1 2017 Phase 3
NCT01812382 Completed Skin Infections Bacterial GlaxoSmithKline April 2 2014 Phase 1
NCT01812382 Completed Skin Infections Bacterial GlaxoSmithKline April 2 2014 Phase 1
NCT01445600 Completed Skin Infections Bacterial GlaxoSmithKline November 2012 --
NCT01445600 Completed Skin Infections Bacterial GlaxoSmithKline November 2012 --

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID