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Home , Retapamulin

Product data sheet MedKoo Cat#: 300270 Name: Retapamulin CAS#: 224452-66-8 Chemical Formula: C30H47NO4S Exact Mass: 517.32258 Molecular Weight: 517.76 Product supplied as: Powder Purity (by HPLC): ≥ 98% Shipping conditions Ambient temperature Storage conditions: Powder: -20°C 3 years; 4°C 2 years. In solvent: -80°C 3 months; -20°C 2 weeks.

1. Product description: Retapamulin, also known as SB-275833, is a newer topical agent of class approved by the Food and Drug Administration for treatment of in children. It has been demonstrated to have low potential for the development of antibacterial resistance and a high degree of potency against poly drug resistant Gram-positive found in skin infections including strains. The drug is safe owing to low systemic absorption and has only minimal side-effect of local irritation at the site of application.

2. CoA, QC data, SDS, and handling instruction SDS and handling instruction, CoA with copies of QC data (NMR, HPLC and MS analytical spectra) can be downloaded from the product web page under “QC And Documents” section. Note: copies of analytical spectra may not be available if the product is being supplied by MedKoo partners. Whether the product was made by MedKoo or provided by its partners, the quality is 100% guaranteed.

3. Solubility data Solvent Max Conc. mg/mL Max Conc. mM DMSO 30.0 57.9 Ethanol 30.0 57.9

4. Stock solution preparation table: Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg 1 mM 1.93 mL 9.66 mL 19.31 mL 5 mM 0.39 mL 1.93 mL 3.86 mL 10 mM 0.19 mL 0.97 mL 1.93 mL 50 mM 0.04 mL 0.19 mL 0.39 mL

5. Molarity Calculator, Reconstitution Calculator, Dilution Calculator Please refer the product web page under section of “Calculator”

6. Recommended literature which reported protocols for in vitro and in vivo study In vitro study 1. Saravolatz LD, Pawlak J, Saravolatz SN, Johnson LB. In Vitro Activity of Retapamulin against Staphylococcus aureus Resistant to Various Antimicrobial Agents. Antimicrob Agents Chemother. 2013 Sep;57(9):4547-4550. doi: 10.1128/AAC.00282-13. Epub 2013 Jun 24. PMID: 23796931; PMCID: PMC3754297. 2. Candel FJ, Morales G, Picazo JJ. In vitro activity of retapamulin against and methicillin-resistant Staphylococcus aureus isolates. Rev Esp Quimioter. 2011 Sep;24(3):127-30. PMID: 21947094.

In vivo study 1. Guo Y, Ramos RI, Cho JS, Donegan NP, Cheung AL, Miller LS. In vivo bioluminescence imaging to evaluate systemic and topical against community-acquired methicillin-resistant Staphylococcus aureus-infected skin wounds in mice. Antimicrob Agents Chemother. 2013 Feb;57(2):855-63. doi: 10.1128/AAC.01003-12. Epub 2012 Dec 3. PMID: 23208713; PMCID: PMC3553733. 2. Rittenhouse S, Singley C, Hoover J, Page R, Payne D. Use of the surgical wound infection model to determine the efficacious dosing regimen of retapamulin, a novel topical . Antimicrob Agents Chemother. 2006 Nov;50(11):3886-8. doi: 10.1128/AAC.00183-06. PMID: 17065626; PMCID: PMC1635196.

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Product data sheet 7. Bioactivity Biological target: 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.

In vitro activity The purpose of this study was to determine the in vitro activity of retapamulin against methicillin-susceptible Staphylococcus aureus (MSSA), methicillin-resistant S. aureus (MRSA), and linezolid and methicillin-resistant S. aureus.The minimum inhibitory concentrations (MICs) were determined on Mueller-Hinton agar. Retapamulin inhibited all the isolates of MSSA and MRSA at 0.125 mg/L, but the 18 linezolid-resistant-MRSA strains proved resistant, with MICs over 32 mg/L. Retapamulin demonstrated excellent in vitro activity against MSSA and MRSA strains, but not against MRSA isolates harbouring the cfr gene. The results of this in vitro study support cut-off values for retapamulin of ≤ 0.5, 1, and ≥ 2 mg/L for susceptible, intermediate, and resistant strains, respectively.

Reference: Rev Esp Quimioter. 2011 Sep;24(3):127-30. https://pubmed.ncbi.nlm.nih.gov/21947094/

In vivo activity The purpose of this study was to evaluate the effect of topically applied retapamulin ointment using various dosing regimens in the Staphylococcus aureus and wound infection model. Therapy was administered topically (0.1 ml/mouse) b.i.d. (beginning at 1 and 7 h postinfection) or t.i.d. (beginning at 1, 4, and 7 h postinfection) and continued for 3, 4, or 6 days (4, 5, or 7 days of therapy). Additional groups of mice received petrolatum ointment or remained untreated to act as placebo or infected controls. Following infection with S. aureus J1225 (5 days postinfection), bacterial numbers from untreated control animals were 6.3 ± 0.3 log10 CFU/wound. Retapamulin administered t.i.d. for 4 days demonstrated significant efficacy (P ≤ 0.01) compared with untreated animals at all concentrations tested. A maximum 4.6 log10 reduction in bacterial counts was achieved at 2% (wt/wt) (1.7 ± 0.1 log10 CFU/wound; 7/8 wounds cleared to the limit of detection). All retapamulin concentrations evaluated produced a potent effect compared with untreated or placebo-treated animals (P ≤ 0.01). The effect obtained with 4-day t.i.d. application of 0.5%, 1%, and 2% wt/wt were similar, reducing bacterial counts by >5 log10 (1.9 ± 0.4, 2.3 ± 1.3, and 2.3 ± 1.5 log10 CFU/wound, respectively). Overall, these results demonstrate the potential benefit of retapamulin over existing topical antibiotics, particularly against isolates resistant to currently used agents.

Reference: Antimicrob Agents Chemother. 2006 Nov; 50(11): 3886–3888. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1635196/

Note: The information listed here was extracted from literature. MedKoo has not independently retested and confirmed the accuracy of these methods. Customer should use it just for a reference only.

MedKoo Biosciences || http://www.medkoo.com || [email protected] 2500 Gateway Centre Blvd Suite 400, Morrisville, NC27560, USA. Tel: 919-636-5577, Fax: 919-980-4831