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
- 화학식: C42H62N6O11S
- 분자량:859.04
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Antibiotic Isoforms
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Biological Activity
제품 설명
In Vitro
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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| 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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분자량 859.04
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- 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