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M6118835

Telithromycin , ≥99% , 191114-48-4

CAS NO.:191114-48-4

Empirical Formula: C43H65N5O10

Molecular Weight: 812

MDL number: MFCD04117983

EINECS: 682-750-4

Pack Size Price Stock Quantity
1mg RMB1328.00 In Stock
5mg RMB3984.00 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 176-188 C
Boiling point: 966℃
Density  1.26±0.1 g/cm3(Predicted)
RTECS  KF4674500
Flash point: >110°(230°F)
storage temp.  Sealed in dry,Store in freezer, under -20°C
solubility  Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
pka 10.85±0.70(Predicted)
form  Solid
color  White to Light Beige
Water Solubility  Sparingly soluble in water

Description and Uses

Telithromycin was first launched in Germany as a once-daily oral treatment for respiratory infections including community-acquired pneumonia, acute bacterial exacerbations of chronic bronchitis, acute sinusitis and tonsillitis/pharyngitis. This semisynthetic derivative of the natural macrolide erythromycin is the first marketed ketolide, a new class of antibiotics featuring a C3-ketone instead of the L-cladinose group. The 14-membered ring antibacterial agent prevents bacterial protein synthesis by binding to two domains of the 50S subunit of bacterial ribosomes. It shows potent in vitro activity against common respiratory pathogens including Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis and Streptococcus pyogenes as well as other atypical pathogens. The 3-keto group confers increased acidic stability and reduced induction of macrolide-lincosamide-streptogramin B resistance that is frequently observed with macrolides. The substituted C11-C12 carbamate residue appears not only to increase affinity for the ribosomal binding site but also to stabilize the compound against esterase hydrolysis and avoid resistance due to elimination of macrolides from the cell by an efflux pump encoded by the mef gene in certain pathogens. Telithromycin is both a competitive inhibitor and a substrate of CYP3A4. However, unlike several macrolides such as troleandomycin, it does not form a stable inhibitory CYP P-450 Fe2+-nitrosoalkane metabolite complex which is potentially hepatotoxic. The drug is well tolerated and well distributed into pulmonary tissues, bronchial secretions, tonsils and saliva. It turns out to be highly concentrated in azurophil granules of polymorphonuclear neutrophils thereby facilitating its delivery to the phagocytosed bacteria.

Telithromycin is a ketolide antibiotic, used to treat respiratory infections

Safety

Symbol(GHS) 
GHS07,GHS09
Signal word  Warning
Hazard statements  H315-H319-H335-H400-H410
Precautionary statements  P261-P280a-P304+P340-P305+P351+P338-P405-P501a
Hazard Codes  Xi
Risk Statements  36/37/38
Safety Statements  26-36
HazardClass  9

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