Upleganan
Based on 1 publication(s) in Google Scholar
Upleganan (SPR206), a polymyxin analogue, and shows antibiotic activity against multidrug resistant Gram-negative pathogen. The MIC values of Upleganan against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L.
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- CAS. Nr.: 2407717-17-1
- Formel: C52H82ClN15O12
- Molecular Weight:1144.75
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Speicherung:
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Biologische Aktivität
MIC: 0.125 mg/L (Pseudomonas aeruginosa Pa14) and 0.125 mg/L (Acinetobacter baumannii NCTC13301[1][2]
Upleganan (SPR206) exhibits strong anti-microbial properties against Gram-negative bacteria. The MIC values of SPR206 against E. coli IHMA558090, E. coli ATCC 25922, K. pneumonia ATCC 13882, P. aeruginosa ATCC 27853, A. baumannii NCTC13424 and A. baumannii ATCC 19003 are 8 mg/L, 0.125 mg/L, 0.125 mg/L, 0.25 mg/L, 0.06 mg/L and 0.125 mg/L, respectively, together with lower cytotoxicity [1].
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.
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Animal Model:Neutropenic mice infected Pa14 or NCTC13301[2]
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Dosage:3 mg/kg, 10 mg/kg, 20 mg/kg, 30 mg/kg (intravenous injection); 0.125 mg/kg, 0.5 mg/kg, 1 mg/kg, 4 mg/kg (subcutaneous injection)
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Administration:Intravenous injection or subcutaneous injection; every 8 hours or every 4 hours; for 16 hours or 24 hours
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Result:In lung tissue, reduced the burden of Pa14 and NCTC13301 by 1.5 and 3.6 log10 CFU/mL. In the thigh model, reduced the burden of Ab13301 by 3.4 and 4.3 log10 CFU/g.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2407717-17-1
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Molecular Weight 1144.75
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Formel C52H82ClN15O12
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SMILES
O=C(N[C@@H](CC(C)C)C(N[C@@H](CCN)C(N[C@@H](CCN)C(N1)=O)=O)=O)[C@H](NC([C@H](CCN)NC([C@H](CCNC([C@@H]1[C@H](O)C)=O)NC([C@H](CN)NC([C@@H](NC(C[C@@H](C2=CC=CC(Cl)=C2)CN)=O)[C@H](O)C)=O)=O)=O)=O)CC3=CC=CC=C3
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Synonyms
SPR206
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Reinheit & Dokumentation
Verweise
[1]. Brown P, et al. Design of Next Generation Polymyxins with Lower Toxicity: The Discovery of SPR206. ACS Infect Dis. 2019 Oct 11;5(10):1645-1656. [Content Brief]
[3]. Noushin Akhoundsadegh, et al. Outer Membrane Interaction Kinetics of New Polymyxin B Analogs in Gram-Negative Bacilli. Antimicrob Agents Chemother. 2019 Sep 23;63(10):e00935-19. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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