Telithromycin

Research use only, not for human use.

Telithromycin is a ketolide antibiotic to treat community acquired pneumonia of mild to moderate severity. Antibacterial Telithromycin prevents bacteria from growing, by interfering with their protein synthesis.

Telithromycin is a ketolide antibiotic to treat community acquired pneumonia of mild to moderate severity. Antibacterial Telithromycin prevents bacteria from growing, by interfering with their protein synthesis. Telithromycin binds to the subunit 50S of the bacterial ribosome, and blocks the progression of the growing polypeptide chain. Telithromycin has over 10 times higher affinity to the subunit 50S than erythromycin. In addition, telithromycin strongly bind simultaneously to two domains of 23S RNA of the 50 S ribosomal subunit, where older macrolides bind strongly only to one domain and weakly to the second domain. Telithromycin can also inhibit the formation of ribosomal subunits 50S and 30S.(In Vitro):Telithromycin (HMR3647) (0-50 μg/mL, 30 min) suppress C. pneumoniae-induced MUC5AC production.Telithromycin (0-50 μg/mL, 30 min) suppress C. pneumoniae-induced NF-kB activation.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.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.(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.

Telithromycin (HMR3647) (0-50 μg/mL, 30 min) suppress C. pneumoniae-induced MUC5AC production.Telithromycin (0-50 μg/mL, 30 min) suppress C. pneumoniae-induced NF-kB activation.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.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:RT-PCR Cell Line:NCI-H292 cells Concentration: 0-50 μg/mL Incubation Time:30 min Result:Suppressed C. 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 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.

Telithromycin (HMR3647) (20 mg/kg, ip., single) reduces protein, nitrite, MIP-2, and TNF-α levels in the BAL fluid of LPS-nebulized animals. Animal Model:LPS-Nebulized MiceDosage: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.

Telithromycin | HMR-3647 | HMR 3647

Endocrinology/Hormones

5-HT Receptor

Antibacterial

Infection

——

191114-48-4

812

C43H65N5O10

>98% (HPLC)

DMSO : ≥ 100 mg/mL; 123.15 mM

CC[C@H]1OC(=O)[C@H](C)C(=O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@@](C)(C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCCCn3cnc(c3)-c3cccnc3)C(=O)O[C@]12C)OC

(3aS,4R,7R,9R,10R,11R,13R,15R,15aR)-10-(((2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-4-ethyl-11-methoxy-3a,7,9,11,13,15-hexamethyl-1-(4-(4-(pyridin-3-yl)-1H-imidazol-1-yl)butyl)octahydro-2H-[1]oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1H,7H,9H)-tetraone

(-20℃)

With Ice Pack

≥ 2 years