Solithromycin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Solithromycin(CEM-101)是一种新型的\有效的以及广谱的氟酮内酯类抗生素[1][2].
抗生素属于抗微生物药,用于治疗和预防细菌感染.
Solithromycin(CEM-101)是一种广谱的氟酮内酯类抗生素.CEM-101有效抑制各种革兰氏阳性与革兰氏阴性细菌,包括支原体\解脲脲原体以及与呼吸道感染和皮肤感染相关的细菌,其MIC50值分别为0.015 μg/mL和4 μg/mL[1].Solithromycin(CEM-101)结合核糖体50S大亚基并抑制蛋白生物合成.在肺炎链球菌\金黄色葡萄球菌以及流感嗜血杆菌中,Solithromycin抑制细胞活力\蛋白合成以及生长速率,其IC50值分别为7.5 ng/ml\40 ng/ml和125 ng/ml.Solithromycin也抑制50S亚基形成[3].在单核细胞系U937细胞中,Solithromycin抑制TNFα/CXCL8合成与MMP9活性.在单核细胞系U937细胞中,Solithromycin(10 μM)显著抑制氧化应激激活的NF-κB活性.在慢性阻塞性肺疾病(COPD)患者的离体PBMC中,Solithromycin(10 μM)抑制TNFα释放以及MMP9活性[4].
在C57BL/6J小鼠中,Solithromycin抑制香烟烟雾诱导的中性粒细胞以及MMP9前体的合成[4].CEM-101作为一种有效的抗微生物药,也用于预防和治疗宫内感染[2].
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 845.01 |
Cas No. | 760981-83-7 |
Formula | C43H65FN6O10 |
Solubility | ≥34.35 mg/mL in DMSO |
Chemical Name | (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 |
SDF | Download SDF |
Canonical SMILES | CC[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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
李斯特菌,淋球菌 |
溶解方法 |
在DMSO中的溶解度≥34.35mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应时间 |
0.015 microg/mL,4 microg/mL |
应用 |
与泰利霉素(MIC(50),0.06 microg / mL),克拉霉素(MIC(50),0.12 microg / mL)和红霉素(MIC(50),0.25 microg / mL)相比,CEM-101(MIC(50),0.015 microg / mL)对所有革兰氏阳性菌具有高活性。在革兰氏阴性菌中,CEM-101(MIC(50),4 microg / mL)还显示出对大多数菌株的高效力,但与在MIC(50)值范围内测试的其他抗菌药物相比,如从左氧氟沙星的0.12 microg / mL到泰利霉素的8 microg / mL范围内,具有同等效力或更低活性。 |
动物实验 [2]: | |
动物模型 |
长期插管的怀孕母羊 |
剂量 |
母体静脉注射(10 mg / kg),羊膜内(ia)注射(1.4 mg / kg) |
应用 |
在给药后0至72小时间隔,通过导管采集母体血浆(MP),胎儿血浆(FP)和羊水(AF)样品,以及确定Solithromycin及其生物活性代谢物(N-乙酰[NAc] -CEM-101和CEM-214的浓度。随着母体静脉注射,血浆、胎儿血浆和羊水中的CEM-101峰值浓度分别为1073、353和214 ng / ml,表明母婴间血浆转移效率为34%。单一母体剂量导致MP,FP和AF中有效浓度(> 30 ng / ml)持续超过12小时。 NAc-CEM-101和CEM-214在FP和AF中显示积累和清除延迟,从而产生了累加的抗菌作用(> 48小时)。尽管羊膜到胎儿的转移效率很低(〜1.5%),羊膜内注射Solithromycin可导致AF中CEM-101的浓度升高(〜50μg/ ml),并且保持FP中较高浓度的CEM-101。我们的发现表明,CEM-101可能首次为预防和治疗宫内感染和及早预防早产提供了有效的抗菌方法。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。 |
References: [1]. Putnam SD, Castanheira M, Moet GJ, Farrell DJ, Jones RN. CEM-101, a novel fluoroketolide: antimicrobial activity against a diverse collection of Gram-positive and Gram-negative bacteria. Diagn Microbiol Infect Dis. 2010 Apr;66(4):393-401. doi: 10.1016/j.diagmicrobio.2009.10.013. PubMed PMID:20022192. [2]. Richards DM, Brogden RN. Ceftazidime. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 1985 Feb;29(2):105-61. Review. PubMed PMID: 3884319. |