Name: Retapamulin
Brand: Selleck Chemicals
SKU: S4056
Availability: InStock
Rating: 5 (3 reviews)

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Quality Control

Batch: Purity: 99.54%

99.54

Related Targets	Integrase Bacterial Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease
Other Antibiotics Inhibitors	G418 Sulfate (Geneticin) Nanchangmycin Fusidine Sitafloxacin Hydrate Gamithromycin Tildipirosin Spiramycin Nadifloxacin 6-Aminopenicillanic acid Thiamphenicol

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (193.13 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (9.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.71mg/ml (1.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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

+

%

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.

Chemical Information, Storage & Stability

Molecular Weight	517.76	Formula	C₃₀H₄₇NO₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	224452-66-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SB-275833			Smiles	CC1CCC23CCC(=O)C2C1(C(CC(C(C3C)O)(C)C=C)OC(=O)CSC4CC5CCC(C4)N5C)C

Mechanism of Action

Features	Retapamulin is insoluble in water but is soluble in dimethyl sulfoxide and methanol.
Targets/IC₅₀/Ki	ribosome ribosome 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. This compound (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. It binds to Erys ribosomes and fully displaces the labeled ligand with an IC50 of 26.1 nM. This agent 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%). It inhibits Staphylococcus aureus and Streptococcus pyogenes with MIC90 of 0.12 μg/mL and ≤0.03 μg/mL, respectively. This chemical inhibits S. aureus subset with MIC50/90 values of 0.06/0.12 μg/mL. It shows excellent activity against these isolates, with only two requiring a MIC of 0.06 μg/mL. It 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. This inhibitor binds to a unique site on the bacterial ribosome, and by virtue of its novel mode of action. This compound (<2 mg/L) inhibits 37/52 (71%) strains of the B. fragilis group and 85/87 (98%) of the other Gram-negative bacilli. It is more active than clindamycin, metronidazole and ceftriaxone against Propionibacterium acnes and anaerobic Gram-positive cocci. It 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16940066/ [2] https://pubmed.ncbi.nlm.nih.gov/16801451/ [3] https://pubmed.ncbi.nlm.nih.gov/17065625/ [4] https://pubmed.ncbi.nlm.nih.gov/17350985/ [5] https://pubmed.ncbi.nlm.nih.gov/17562806/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03304873	Completed	MRSA	NYU Langone Health	December 1 2017	Phase 3
NCT01812382	Completed	Skin Infections Bacterial	GlaxoSmithKline	April 2 2014	Phase 1
NCT01445600	Completed	Skin Infections Bacterial	GlaxoSmithKline	November 2012	--
NCT00903279	Withdrawn	Orthopedic Procedures\|Methicillin-resistant Staphylococcus Aureus	Bay Pines VA Healthcare System	August 2009	Phase 2

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Retapamulin Antibiotics chemical

Chemical Structure

Molecular Weight: 517.76