YU253434
YU253434 is a PBP3 inhibitor with an IC50 of 2.5 μM against Pseudomonas aeruginosa PBP3. YU253434 contains a siderophore domain that facilitates its uptake into the periplasmic space of Gram-negative bacilli. YU253434 exhibits antibacterial activity against multidrug-resistant Gram-negative bacilli. YU253434 can be used in studies of multidrug-resistant Gram-negative bacterial infections.
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- No. CAS: 2408801-88-5
- Fòrmula: C27H26N8O12S
- Peso molecular:686.61
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
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Help & FAQs
Actividad biológica
YU253434 potently inhibits growth of clinical isolates of Pseudomonas aeruginosa (MIC50 = 1 μg/mL, MIC90 = 8 μg/mL), Klebsiella pneumoniae (MIC50 = 1 μg/mL, MIC90 = 4 μg/mL), and Escherichia coli (MIC50 = 1 μg/mL, MIC90 = 4 μg/mL), with antimicrobial activity decreasing in a concentration-dependent manner with increasing media iron levels[1].
YU253434 is resistant to hydrolysis by class A, C, and D serine β-lactamases, and is a poor substrate for class B metallo-β-lactamases NDM-1, VIM-2, and IMP-1, with kcat/Km values 36-335-fold lower than imipenem[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | C0 | AUClast | AUCinf | MRT | Vss | CL |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 50 mg/kg | i.v. | 11 h | 200844 ng/mL | 55866 ng·h/mL | 57791 ng·h/mL | 3 h | 2 L/kg | 14 mL/min/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:50 mg/kg (i.v.); 50 mg/kg (s.c.)
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Administration:i.v.; single dose; s.c.; single dose
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Result:Reached plasma concentration of 1395 ng/mL at 4 hours after intravenous administration.
Maintained plasma concentration above 1000 ng/mL at the 2-hour time point after intravenous administration.
Achieved a half-life of 11 h, initial plasma concentration (C0) of 200844 ng/mL, AUClast of 55866 h ng/mL, AUCINF of 57791 h ng/mL, mean residence time (MRT) of 3 h, volume of distribution at steady state (Vss) of 2 L/kg, and clearance (CL) of 14 mL/min/kg after intravenous administration.
Yielded nearly identical pharmacokinetic data after subcutaneous administration.
Chemical Information
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No. CAS 2408801-88-5
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Peso molecular 686.61
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Fòrmula C27H26N8O12S
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SMILES
OC(C1=C(C(NCCN2C(C3=CC(O)=C(O)C=C3C2=O)=O)=O)CN(C[C@@H]4NC(/C(C5=CSC(N)=N5)=N\OC(C)(C)C(O)=O)=O)N1C4=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YU253434 Related Classifications
HY-182396 Related Classifications
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