Nafithromycin
Nafithromycin (WCK 4873) is an orally active ketolide antibiotic with activity against Gram-positive bacteria, Gram-negative bacteria, and atypical respiratory pathogens (including drug-resistant strains). Nafithromycin binds to domains II and V of bacterial 23S rRNA and the peptidyl transferase center of the 50S ribosomal subunit, thereby inhibiting protein synthesis. Nafithromycin can be used in research related to bacterial infections.
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- CAS No.: 1691240-78-4
- Formule: C42H62N6O11S
- Masse moléculaire:859.04
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Nafithromycin (0.03-1 mg/liter; 72 h) exhibits in vitro activity against 10 clinical Chlamydia pneumoniae isolates, with an MIC50 of 0.03 mg/liter and an MIC90 of 0.25 mg/liter[1].
Nafithromycin (WCK 4873) potently inhibits growth of erythromycin-sensitive, mef-expressing, ermB-expressing, and high-level ermB-expressing Streptococcus pneumoniae, as well as high-level ermB-expressing Streptococcus pyogenes, with MICs ranging from 0.015-0.03 μg/mL to 0.5 μg/mL[2].
Nafithromycin shows non-cytotoxic effects up to 62.5 μg/mL in CHO cells, 31.25 μg/mL in MDBK, V79, HepG2, L929, and HeLa cells, and 15.6- ≤ 31.25 μg/mL in J774 cells[2].
Nafithromycin exhibits potent in vitro activity against Streptococcus pneumoniae (MIC50/MIC90 0.015/0.06 μg/mL, 100% inhibited at ≤0.25 μg/mL), Streptococcus pyogenes (MIC50/MIC90 0.015/0.015 μg/mL, 100% inhibited at ≤0.5 μg/mL), and Moraxella catarrhalis (MIC50/MIC90 0.12/0.25 μg/mL), bimodal activity against Staphylococcus aureus (MIC50/MIC90 0.06/>2 μg/mL), and moderate activity against Haemophilus influenzae (MIC50/MIC90 4/4 μg/mL) when tested against 2014 global clinical respiratory isolates via CLSI broth microdilution methods[3].
Nafithromycin potently inhibits clinical Streptococcus pneumoniae isolates (including macrolide-resistant strains) with an MIC50 of 0.03 mg/L and MIC90 of 0.06 mg/L, and achieves 100% susceptibility at a PK/PD breakpoint of 0.25 mg/L[4].
Nafithromycin potently inhibits Indian clinical Streptococcus pneumoniae isolates (including those with erm and mef-mediated macrolide resistance) with an MIC50 of 0.015 mg/L and MIC90 of 0.06 mg/L[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1691240-78-4
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Masse moléculaire 859.04
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Formule C42H62N6O11S
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SMILES
C[C@@]12[C@]([C@H](C([C@@H](C[C@](C)([C@@H]([C@H](C([C@H](C(O[C@@H]2CC)=O)C)=O)C)O[C@H]3[C@@H]([C@H](C[C@H](O3)C)N(C)C)O)OC)C)=O)C)([H])[C@@H](C(O1)=O)/C(N)=N/O[C@H](C4=NN=C(C5=CC=CC=N5)S4)C
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Synonyms
WCK 4873
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Nafithromycin
- 1691240-78-4
- WCK 4873
- WCK4873
- WCK-4873
- Antibiotic
- Bacterial
- peptidyl transferase center
- 23S rRNA
- 50S ribosomal subunit
- Gram-negative pathogens
- atypical respiratory pathogens
- Streptococcus pyogenes
- community-acquired bacterial pneumonia
- Chlamydia pneumoniae
- Streptococcus pneumoniae
- Gram-positive pathogens
- Inhibitor
- inhibitor
- inhibit