Retapamulin

製品コードS4056 バッチS405602

化学情報

	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	100 mg/mL (193.13 mM)
		Water	Insoluble
* <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 K_d 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. 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]
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
キナーゼアッセイ	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 Retapamulin 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 retapamulin 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

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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。

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