Retapamulin

製品コードS4056 バッチS405603

印刷

化学情報

Chemical Structure Synonyms SB-275833 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C30H47NO4S
分子量 517.76 CAS No. 224452-66-8
Solubility (25°C)* 体外 DMSO 100 mg/mL (193.13 mM)
Ethanol 50 mg/mL (96.56 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
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 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 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 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 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. 
* <1 mg/ml means slightly soluble or 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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 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%). [1] 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. [2] 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. [3] 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. [4] 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. [5]
特徴 Retapamulin is insoluble in water but is soluble in dimethyl sulfoxide and methanol.

プロトコル(参考用のみ)

キナーゼアッセイ Kd determination of retapamulin binding to ribosomes from E. coli and Staphylococcus aureus
Bacterial ribosomes are incubated at 37℃ for 15 min before dilution in binding buffer (20 mM HEPES, pH 7.5, 50 mM NH4Cl, 10 mM MgCl2, 0.05% Tween 20; for S. aureus ribosomes, this buffer contained 25 mM MgCl2). The on rate and off rate of retapamulin binding to both E. coli and S. aureus ribosomes is investigated in the presence of a radiolabeled pleuromutilin ([3H]SB-258781) in a 96-well plate. In these experiments (n = 3), 20 nM this compound is mixed with ribosomes (5 nM to 15 nM) and [3H]SB-258781 (15 to 19 nM) in a final volume of 100 μL. The binding of [3H]SB-258781 to the ribosomes is competed with this chemical at room temperature over a time course (2 hours for E. coli ribosomes and 5 hours for S. aureus ribosomes). The free and bound ligands are then separated through a filter plate using a cell harvester. The plate is allowed to dry at 50℃ for 30 min. After the addition of 50 μL of MicroScint-20 to the plate, the radioactivity in the plate is measured using a TopCount. Nonspecific binding is determined by displacement of [3H]SB-258781 with 10 μM SB-268091.

参考

  • https://pubmed.ncbi.nlm.nih.gov/16940066/
  • https://pubmed.ncbi.nlm.nih.gov/16801451/
  • https://pubmed.ncbi.nlm.nih.gov/17065625/
  • https://pubmed.ncbi.nlm.nih.gov/17350985/
  • https://pubmed.ncbi.nlm.nih.gov/17562806/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Efficacy of a Novel Antibacterial Agent Exeporfinium Chloride, (XF-73), Against Antibiotic-Resistant Bacteria in Mouse Superficial Skin Infection Models [ Infect Drug Resist, 2023, 16:4867-4879] PubMed: 37520450
Efficacy of a Novel Antibacterial Agent Exeporfinium Chloride, (XF-73), Against Antibiotic-Resistant Bacteria in Mouse Superficial Skin Infection Models [ Infect Drug Resist, 2023, 16:4867-4879] PubMed: 37520450
Retapamulin Activity Against Pediatric Strains of Mupirocin-resistant Methicillin-resistant Staphylococcus aureus [ Pediatr Infect Dis J, 2021, 40(7):637-638] PubMed: 33657598
Drug repositioning as a therapeutic strategy for neurodegenerations associated with OPA1 mutations [ Hum Mol Genet, 2020, ddaa244] PubMed: 33231680

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。