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.
For research use only. We do not sell to patients.
- CAS No.: 2407717-17-1
- Formula: C52H82ClN15O12
- Molecular Weight:1144.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Upleganan
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Biological Activity
Description
IC50 & Target
MIC: 0.125 mg/L (Pseudomonas aeruginosa Pa14) and 0.125 mg/L (Acinetobacter baumannii NCTC13301[1][2]
In Vitro
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. Further protocols information, click here.
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2407717-17-1
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Molecular Weight 1144.75
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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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.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)