| 產(chǎn)品描述： | Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis |
| 靶點： |
Macrolide;Antibacterial;Antibiotic |
| 體外研究： |
The IC50s values for Solithromycin on TNFα and CXCL8 release are 41.6 μM and 78.2 μM, respectively. Solithromycin markedly reduces MMP9 activity, with an IC50 of 14.9 μM. Solithromycin (0-333 μM; 72 hours; U937 and PBMC cells) suppresses lipopolysaccharide-induced TNFα release and phorbol 12-myristate 13-acetate (PMA)-induced matrix metalloproteinase 9 (MMP9) activity, and does not affect cell viability in monocytic U937 and PBMC cells |
| 體內(nèi)研究： |
Solithromycin (100 mg/kg; oral administration; every day; for 8 days; C57BL/6J mice) treatment inhibits inflammatory cells accumulation and pro-MMP9 production in cigarette smoke-exposed mice. Animal Model: C57BL/6J mice (male, 4 weeks) Dosage: 100 mg/kg Administration: Oral administration; every day; for 8 days Result: Inhibited cigarette smoke-induced neutrophilia and pro-MMP9 production. |
| 參考文獻： |
1. Rodgers W, et al. Solithromycin inhibition of protein synthesis and ribosome biogenesis in Staphylococcus aureus,Streptococcus pneumoniae, and Haemophilus influenzae. Antimicrob Agents Chemother. 2013 Apr;57(4):1632-1637. 2. Kobayashi Y, et al. A novel macrolide solithromycin exerts superior anti-inflammatory effect via NF-κB inhibition. J Pharmacol Exp Ther. 2013 Apr;345(1):76-84. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.183 ml |
5.917 ml |
11.834 ml |
| 5 mM |
0.237 ml |
1.183 ml |
2.367 ml |
| 10 mM |
0.118 ml |
0.592 ml |
1.183 ml |
| 50 mM |
0.024 ml |
0.118 ml |
0.237 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京