2. Anti-infection
  3. Penicillin-binding protein (PBP) Bacterial
  4. 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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YU253434

YU253434 Chemical Structure

CAS No. : 2408801-88-5

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YU253434 Related Antibodies

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Description

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[1].

In Vitro

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.

YU253434 Related Antibodies
Parmacokinetics
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
In Vivo

YU253434 (50 mg/kg; i.v., s.c.; single dose) exhibits rapid clearance similar to intravenous β-lactam antibiotics in CD-1 mice, with plasma levels maintained above its MIC50 of 1 μg/mL for at least 2 hours after a single 50 mg/kg intravenous dose[1].

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

Animal Model: CD-1 mice[1]
Dosage: 50 mg/kg (i.v.); 50 mg/kg (s.c.)
Administration: i.v.; single dose; s.c.; single dose
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.
Molecular Weight

686.61

Formula

C27H26N8O12S
CAS No.
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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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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YU253434 Related Classifications

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  • Do most proteins show cross-species activity?

    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.

Keywords:

YU2534342408801-88-5YU 253434YU-253434Penicillin-binding protein (PBP)Bacterialcatalytic serine residuePBP3Klebsiella pneumoniaeserine β-lactamasesmetallo-β-lactamasesEscherichia coliGram-negative bacilliβ-lactamasesPseudomonas aeruginosasiderophore moietyInhibitorinhibitorinhibit

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