Telithromycin (HMR3647) 是一种结构类似大环内酯类的新型酮内酯类抗生素。Telithromycin 属于酮内酯家族，其特征是大环 3 位的酮群，对引起社区获得性肺炎、慢性支气管炎急性加重和急性鼻窦炎的细菌有活性。Telithromycin 也具有与大环内酯类相似的免疫调节作用。Telithromycin 可用于支气管哮喘等呼吸道感染的研究。
| 生物活性 | Telithromycin (HMR3647) is a novelketolideantibioticthat structurally resembles macrolides. Telithromycin belongs to the ketolide family that is characterized by a keto group at position 3 of themacrolidering and is active against bacteria causing community-acquired pneumonia, acute exacerbation of chronic bronchitis, and acute sinusitis. Telithromycin also has similar immunomodulatory effects as macrolides. Telithromycin can be used for the research of respiratory infections including bronchial asthma[1][2]. |
| IC50& Target | |
体外研究
(In Vitro) | Telithromycin (HMR3647) (0-50 μg/mL, 30 min) suppressC. pneumoniae-induced MUC5AC production[1].
Telithromycin (0-50 μg/mL, 30 min) suppressC. pneumoniae-induced NF-kB activation[1].
Telithromycin (10 mg/mL, 1 h) inhibits the production of MIP-2 and TNF-α in a dose-dependent manner by LPS-stimulated RAW 264.7 macrophages[2].
Telithromycin (10 mg/mL, 1 h) inhibits NF-kB activation, increases apoptosis in cell and decreases the LPS-induced influx of neutrophils in BAL fluid[2].
RT-PCR[1] | Cell Line: | NCI-H292 cells | | Concentration: | 0-50 μg/mL | | Incubation Time: | 30 min | | Result: | SuppressedC. pneumoniae-induced MUC5AC production in dose-dependently and significantly decreased MUC5AC production at 50 mg/mL.
Suppressed p65 and p50 activation in NCI-H292 cells. |
Apoptosis Analysis[2] | Cell Line: | RAW 264.7 and MLE-12 cells | | Concentration: | 10 mg/mL | | Incubation Time: | 1 h | | Result: | Increased the apoptotic activity in cells induced with supernatants from LPS-treated RAW 264.7 macrophages and in LPS-induced cells. |
|
体内研究
(In Vivo) | Telithromycin (HMR3647) (20 mg/kg, ip., single) reduces protein, nitrite, MIP-2, and TNF-α levels in the BAL fluid of LPS-nebulized animals[2].
| Animal Model: | LPS-Nebulized Mice[2] | | Dosage: | 20 mg/kg | | Administration: | 20 mg/kg, ip., single | | Result: | Increased the protein concentration, reduced the concentrations of nitrite and the levels of TNF-α and induced significant reductions the levels of MIP-2. |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(123.15 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.2315 mL | 6.1576 mL | 12.3153 mL | | 5 mM | 0.2463 mL | 1.2315 mL | 2.4631 mL | | 10 mM | 0.1232 mL | 0.6158 mL | 1.2315 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (3.08 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.08 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (3.08 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.08 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.08 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
