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Solithromycin
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。
Solithromycin图片
CAS NO:760981-83-7
包装与价格：
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
Solithromycin (CEM-101) 是一种口服生物可利用的有效抗菌剂，抑制细胞活力、蛋白质合成和生长速率的 IC50 分别为 7.5 ng/mL、40 ng/mL 和 125 ng/mL，对肺炎链球菌、葡萄球菌分别为金黄色葡萄球菌和流感嗜血杆菌。
Cas No.760981-83-7
别名索利霉素; CEM-101; OP-1068
化学名(3aS,4R,7S,9S,10R,11S,13R,15R,15aR)-1-(4-(4-(3-aminophenyl)-1H-1,2,3-triazol-1-yl)butyl)-10-(((2R,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-4-ethyl-7-fluoro-11-methoxy-3a,7,9,11,13,15-hexamethyloctahydro-1H-[1]oxacyclotet
Canonical SMILESCC[C@](O1)([H])[C@@]2([C@@](N(C(O2)=O)CCCCN3C=C(N=N3)C4=CC(N)=CC=C4)([H])[C@@](C([C@](C[C@@]([C@@](O[C@]5([H])[C@@](O)([H])[C@](N(C)C)([H])C[C@@](O5)([H])C)([H])[C@](C([C@@](C1=O)(F)C)=O)([H])C)(OC)C)([H])C)=O)([H])C)C
分子式C43H65FN6O10
分子量845.01
溶解度≥ 34.35mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Solithromycin (CEM-101) is a new, potent and broad-spectrum fluoroketolide antibiotic [1][2].

Antibiotic is an antimicrobial used in the treatment and prevention of bacterial infection.

Solithromycin (CEM-101) is a broad-spectrum fluoroketolide antibiotic. CEM-101 exhibited high potency against diverse groups of Gram-positive and Gram-negative bacteria, including mycoplasma and ureaplasma, as well as bacteria associated with respiratory tract infections and skin infections, with MIC50 values of 0.015 μg/mL and 4 μg/mL, respectively [1]. Solithromycin (CEM-101) bound to the large 50S subunit of the ribosome and inhibited protein biosynthesis. In Streptococcus pneumoniae, Staphylococcus aureus, and Haemophilus influenzae, solithromycin inhibited cell viability, protein synthesis, and growth rate with IC50 values of 7.5, 40, and 125 ng/ml. Solithromycin also inhibition the formation of the 50S subunit [3]. In monocytic U937 cells, solithromycin inhibited TNFα/CXCL8 production and MMP9 activity. In PBMC isolated from chronic obstructive pulmonary disease (COPD) patients, solithromycin (10 μM) inhibited TNFα release and MMP9 activity. In monocytic U937 cells, solithromycin (10 μM) significantly inhibited NF-κB activity activated by oxidative stress [4].

In C57BL/6J mice, solithromycin also inhibited cigarette smoke-induced neutrophilia and pro-MMP9 production [4]. CEM-101 was also an effective antimicrobial for the prevention and treatment of intrauterine infection [2].

References:
[1].  Putnam SD, Castanheira M, Moet GJ, et al. CEM-101, a novel fluoroketolide: antimicrobial activity against a diverse collection of Gram-positive and Gram-negative bacteria. Diagn Microbiol Infect Dis, 2010, 66(4): 393-401.
[2].  Keelan JA, Kemp MW, Payne MS, et al. Maternal administration of solithromycin, a new, potent, broad-spectrum fluoroketolide antibiotic, achieves fetal and intra-amniotic antimicrobial protection in a pregnant sheep model. Antimicrob Agents Chemother, 2014, 58(1): 447-454.
[3].  Rodgers W, Frazier AD, Champney WS. Solithromycin inhibition of protein synthesis and ribosome biogenesis in Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae. Antimicrob Agents Chemother, 2013, 57(4): 1632-1637.
[4].  Kobayashi Y, Wada H, Rossios C, et al. A novel macrolide solithromycin exerts superior anti-inflammatory effect via NF-κB inhibition. J Pharmacol Exp Ther, 2013, 345(1): 76-84.