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Retapamulin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Retapamulin图片
CAS NO:224452-66-8
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
瑞他莫林
SB-275833
产品介绍
Retapamulin是一种能结合金黄色葡萄球菌和大肠杆菌核糖体的局部抗生素,Kd为3 nM。

产品描述

Retapamulin, a Pleuromutilin Antibacterial, binds to both E. coli and S. aureus ribosomes with similar potencies (Kd: 3 nM).

体外活性

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]

Cas No.

224452-66-8

分子式

C30H47NO4S

分子量

517.76

别名

瑞他莫林;SB-275833

储存和溶解度

Ethanol:104 mg/mL (200.86 mM)
DMSO:104 mg/mL (200.86 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years