1. Anti-infection
  2. Bacterial
  3. Upleganan

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (SPR206 acetate) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Upleganan Chemical Structure

Upleganan Chemical Structure

CAS No. : 2407717-17-1

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Description

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[1][2].

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.

In Vivo

Upleganan (SPR206) (0.125-30 mg/kg; intravenous injection or subcutaneous injection; every 8 hours or every 4 hours; for 16 hours or 24 hours; neutropenic mice) treatment reduces the burden of Pa14 and NCTC13301 in lung tissue and in the thigh model[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Neutropenic mice infected Pa14 or NCTC13301[2]
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)
Administration: Intravenous injection or subcutaneous injection; every 8 hours or every 4 hours; for 16 hours or 24 hours
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
Molecular Weight

1144.75

Formula

C52H82ClN15O12

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Upleganan Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Upleganan
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HY-128780
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