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Telithromycin

BVT-0456-M001 1 mg $80.00
BVT-0456-M010 10 mg $180.00
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Additional Information

Product Data
Synonyms RU 66647; Ketek; HMR 3647
Properties
Formula C43H65N5O10
MW 812.0
CAS 191114-48-4
RTECS HB7878000
Source/Host Chemicals Semi-synthetic.
Purity ≥98% (NMR, TLC)
Appearance White solid.
Solubility Soluble in DMSO, ethanol, methanol, acetone or methylene chloride. Sparingly soluble in water (0.3mg/ml).
Identity Determined by 1H-NMR.
Origin Manufactured by BioViotica.
InChi Key LJVAJPDWBABPEJ-XLSPMWLOSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage +4°C
Handling Advice Protect from light when in solution.
Use/Stability Stable for at least 1 year after receipt when stored at +4°C.
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Product Description

  • Ketolide type macrolide antibiotic.
  • Antibacterial compound used to treat mild to moderate respiratory infections.
  • Protein synthesis inhibitor, by binding to the 50S ribosomal subunit and subsequently blocking the progression of the growing polypeptide chain. Binds to domains II and V of the 23S rRNA of the 50S ribosomal subunit.
  • Has a higher affinity for these ribosomal targets than conventional macrolides due to the additional interactions and increased binding at domain II. Retains activity against Gram-positive cocci in the presence of resistance mediated by methylases (erm genes) that alter the binding site at domain V.
  • May inhibit the formation of ribosomal subunits 50S and 30S.

Product References

  1. The ketolide antibiotics HMR-3647 and HMR 3004 are active against Toxoplasma gondii in vitro and in murine models of infection: F.G. Araujo, et al.; Antimicrob. Agents Chemother. 41, 2137 (1997)
  2. The in-vitro activity of HMR 3647, a new ketolide antimicrobial agent: F.J. Boswell, et al.; J. Antimicrob. Chemother. 42, 703 (1998)
  3. Drugs of the 21st century: telithromycin (HMR 3647) - the first ketolide: G. Ackermann & A.C. Rodloff; J. Antimicrob. Chemother. 51, 497 (2003)
  4. Telithromycin: K. Wellington & S. Noble; Drugs 64, 1683 (2004)
  5. Telithromycin: A ketolide antibiotic for treatment of respiratory tract infections: J.R. Lonks & D.A. Goldmann; Clin. Inf. Dis. 40, 1657 (2005)
  6. Antibacterial drug discovery-Then, now and the genomics future: R. Monaghan & J.F. Barrett; Biochem. Pharmacol. 71, 901 (2006)
  7. Telithromycin in the treatment of pneumococcal community-acquired respiratory tract infections: a review: C.M. Fogarty, et al.; Int. J. Infect. Dis. 10, 136 (2006)
  8. Benefit-risk assessment of telithromycin in the treatment of community-acquired pneumonia: S.D. Brown; Drug Safety 31, 561 (2008)
  9. Time-dependent effects of Klebsiella pneumonia endotoxin on the telithromycin pharmacokinetics in rats; restoration of the parameters in 96-hour KPLPS rats to the control levels: J.H. Lee, et al.; Pulm. Pharmacol. Ther. 21, 860 (2008)
  10. Ketolides - the modern relatives of macrolides: the pharmacokinetic perspective: M. Zeitlinger, et al.; Clin. Pharmacokinet. 48, 23 (2009)
  11. Inducible expression of erm(B) by the ketolides telithromycin and cethromycin: P. Byoungduck & M. Yu-Hong; Int. J. Antimicrob. Agents 46, 226 (2015)
  12. ClpP-independent function of ClpX interferes with telithromycin resistance conferred by msr(A) in Staphylococcus aureus: V. Vimberg, et al.; Antimicrob. Agents Chemother. 59, 3611 (2015)
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