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> Retapamulin [224452-66-8]

Retapamulin [224452-66-8]

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Référence HY-17010-10mg

Conditionnement : 10mg

Marque : MedChemExpress

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Description

Retapamulin (SB-275833) is a topical antibiotic that binds Staphylococcus aureus and E. coli ribosomes with a Kd of 3 nM. Retapamulin can be used in researches of atopic dermatitis and prostate cancer[1][2][8].

Cellular Effect
Cell Line Type Value Description References
A549 CC50
>100 μM
Compound: Retapamulin
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
[PMID: 37051724]
A549 CC50
74.17 μM
Compound: Retapamulin
Cytotoxicity against human A549 cells incubated for 24 hrs by CCK8 assay
Cytotoxicity against human A549 cells incubated for 24 hrs by CCK8 assay
[PMID: 37531743]
HEK293 CC50
62.89 μM
Compound: Retapamulin
Cytotoxicity against HEK293 cells incubated for 24 hrs by CCK8 assay
Cytotoxicity against HEK293 cells incubated for 24 hrs by CCK8 assay
[PMID: 37531743]
HEK293 CC50
83.76 μM
Compound: Retapamulin
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
[PMID: 37051724]
HepG2 CC50
36.48 μM
Compound: Retapamulin
Cytotoxicity against human HepG2 cells incubated for 24 hrs by CCK8 assay
Cytotoxicity against human HepG2 cells incubated for 24 hrs by CCK8 assay
[PMID: 37531743]
HepG2 CC50
76.52 μM
Compound: Retapamulin
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
[PMID: 37051724]
HUVEC CC50
25.5 μg/mL
Compound: Retapamulin
Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 37192339]
HUVEC IC50
25.5 μg/mL
Compound: Ratapamulin
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 36549113]
In Vitro

Retapamulin demonstrates excellent in vitro activity against Methicillin (HY-121544)-susceptible Staphylococcus aureus and Methicillin-resistant S. aureus (MRSA) strains, but not against MRSA isolates harbouring the cfr gene[3].
Retapamulin inhibits Streptococcus pyogenes isolates, with MICs ranging from ≤0.015 to 0.12 μg/mL[4].
Retapamulin inhibits Staphylococcus aureus and Streptococcus pyogenes, with MIC90s of 0.12 and ≤0.03 μg/mL, respectively[5].
Retapamulin inhibits total viable cell (TVC), protein synthesis and 50S subunit synthesis of wild-type Staphylococcus aureus strain RN1786 with IC50s of 12 , 5 and 27 ng/mL, respectively[6].
Retapamulin inhibits cytopathic effect, papain-like protease, and MPRO enzymes of SARS-CoV-2 with IC50 values of 4.23, 0.88 and 1.25 µM[7].
Retapamulin (0-10 μM, 3 days) inhibits cell invasion by more than 50% at 0.1 μM in PC-3-KQ cells[8].
Retapamulin (0-500 μg/mL, 16 h) shows cytotoxicity in BRL-3A cells, with an IC50 of 49 μg/mL[9].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Retapamulin Related Antibodies
In Vivo

Retapamulin (1%, applied topically to the lesion area, twice daily for 3 days or 6 days) reduces meticillin-resistant Staphylococcus aureus (MRSA) loads in a murine superficial skin wound infection model[10].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Murine superficial skin wound infection model (abrasive paper was used to induce a minor superficial skin wound on a 1 cm2 area, which was inoculated with 7 log10 CFU of bacteria)[10]
Dosage: 1%
Administration: Applied topically to the lesion area, twice daily for 3 days or 6 days
Result: Reduced the bacterial loads by 2.5 and 5 log10 CFU for 3 days and 6 days, respectively.
Essai clinique
Masse moléculaire

517.76

Formule

C30H47NO4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H]1[C@]23[C@](C(CC3)=O)(08)[C@]([C@H](OC(CS[C@@H]4C[C@@H]5N(C)[C@@H](CC5)C4)=O)C[C@](C=C)(C)[C@H]1O)([C@H](C)CC2)C
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité
In Vitro: 

DMSO : 110 mg/mL (212.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9314 mL 9.6570 mL 19.3140 mL
5 mM 0.3863 mL 1.9314 mL 3.8628 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.75 mg/mL (5.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (5.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Pureté et documentation
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