1. Anti-infection
  2. Bacterial Antibiotic
  3. Cefpirome sulfate

Cefpirome sulfate  (Synonyms: HR-810 sulfate)

Cat. No.: HY-B1824 Purity: 99.49%
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Cefpirome (HR-810) sulfate is a cephalosporin antibiotic that can cross cell membranes and the blood-brain barrier. Cefpirome sulfate binds to penicillin-binding proteins with high affinity, thereby inhibiting bacterial cell wall synthesis. Cefpirome sulfate exhibits bactericidal and growth-inhibitory activities against Gram-negative bacteria, Gram-positive bacteria, and susceptible anaerobic bacteria (including some β-lactamase-producing strains).

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

Cefpirome sulfate

Cefpirome sulfate Chemical Structure

CAS No. : 98753-19-6

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Cefpirome (HR-810) sulfate is a cephalosporin antibiotic that can cross cell membranes and the blood-brain barrier. Cefpirome sulfate binds to penicillin-binding proteins with high affinity, thereby inhibiting bacterial cell wall synthesis. Cefpirome sulfate exhibits bactericidal and growth-inhibitory activities against Gram-negative bacteria, Gram-positive bacteria, and susceptible anaerobic bacteria (including some β-lactamase-producing strains)[1][2][3].

IC50 & Target

β-lactam

 

In Vitro

Cefpirome sulfate exhibits excellent in vitro antibacterial activity against most Enterobacteriaceae (including strains resistant to third-generation cephalosporins), methicillin-sensitive staphylococci, and streptococci (including penicillin-resistant Streptococcus pneumoniae). It shows moderate activity against Pseudomonas aeruginosa, variable activity against anaerobes, and weak activity against methicillin-resistant staphylococci and Enterococcus faecalis[1].
Cefpirome sulfate is stable to most plasmid-mediated and chromosome-mediated β-lactamases, except for extended-spectrum SHV enzymes, and retains activity against β-lactamase-producing, third-generation cephalosporin-resistant *Enterobacteriaceae* strains[1].
Cefpirome sulfate exhibits rapid outer membrane permeability to Gram-negative bacteria, as well as high-affinity binding to key penicillin-binding proteins in both Gram-negative and Gram-positive bacteria, which endows it with broad-spectrum antibacterial activity[1].
Cefpirome (18 h) sulfate exhibits mutation prevention concentration (MPC) against Enterobacter cloacae of 1 μg/mL, which defines a narrow mutant selection window between its MIC (0.125 μg/mL) and MPC[2].
Cefpirome (0.06-32 μg/mL; 18-24 h) sulfate potently inhibits clinical isolates of Enterobacteriaceae (with MIC90 ≤ 0.5 μg/mL for most species), exhibits activity against non-glucose-fermenting Gram-negative bacilli, and shows activity against both oxacillin-susceptible and Oxacillin (HY-B0925A)-resistant staphylococci (the MIC90 is 1 μg/mL for Oxacillin-susceptible Staphylococcus aureus and 16 μg/mL for Oxacillin-resistant Staphylococcus aureus). Only the MIC against coagulase-negative staphylococci shows a slight salt-dependent increase[3].

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

Parmacokinetics
Species Dose Route Vss T1/2 CL
Rat[2] 0.4, 0.8, 1.6, 3.1, 6.3, 12.5, 25, 50 mg/kg i.m. 0.36 L/kg 1.22-1.63 h 1.23-1.64 mL/min
In Vivo

Cefpirome sulfate (0.37 mg/kg) exhibits potent in vivo activity against MSSA-induced acute lethal systemic infection in mice, with an ED50 of 0.37 mg/kg[1].
Cefpirome sulfate (0.025-1.56 mg/kg) demonstrates high in vivo efficacy against a range of bacterial systemic infections in mice, with ED50 values ranging from 0.025 to 1.56 mg/kg[1].
Cefpirome sulfate shows in vivo activity against Pseudomonas aeruginosa-induced systemic infection in mice, but is approximately 2-fold less potent than ceftazidime[1].
Cefpirome sulfate exhibits in vivo efficacy against Acinetobacter spp.-induced systemic infection in mice[1].
Cefpirome sulfate (15.4 mg/kg) is highly bactericidal against Klebsiella pneumoniae-induced pneumonia in mice, with an ED50 of 15.4 mg/kg at 18 hours[1].
Cefpirome (0.4-50 mg/kg b.i.d.; intramuscular injection; every 12 hours; 18 days) sulfate results in dose-dependent survival of rats with K. pneumoniae pneumonia and only minimal selection of stable derepressed ampD-mutated E. cloacae mutants from intestinal flora[2].

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

Animal Model: RP/AEur/RijHsd rats (male, 11-15 weeks old, 250-350 g, left-sided unilateral pneumonia induced via tracheal cannulation with Klebsiella pneumoniae ATCC 43816)[2]
Dosage: 0.4 mg/kg b.i.d.; 0.8 mg/kg b.i.d.; 1.6 mg/kg b.i.d.; 3.1 mg/kg b.i.d.; 6.3 mg/kg b.i.d.; 12.5 mg/kg b.i.d.; 25 mg/kg b.i.d.; 50 mg/kg b.i.d.
Administration: intramuscular injection; every 12 hours; 18 days
Result: Achieved 45% survival rate at day 43 post-inoculation with 3.1 mg/kg b.i.d.
dose.
Achieved 60% survival rate at day 43 post-inoculation with 6.3 mg/kg b.i.d.
dose.
Achieved 100% survival rate at day 43 post-inoculation with 12.5 mg/kg b.i.d.
dose.
Resulted in 50% survival at 12.5 mg/kg/day dose and 90% survival at 25 mg/kg/day dose.
Reduced cefpirome-susceptible intestinal E.
cloacae counts in a dose-dependent manner, with significant reductions (p < 0.05) observed at day 36 for 25 and 50 mg/kg b.i.d., day 29 for 6.3 and 12.5 mg/kg b.i.d., and day 22 for 3.1 mg/kg b.i.d.
compared to pre-treatment levels.
Showed a significant negative correlation between %fT>MIC and log10 cfu counts of susceptible E.
cloacae at days 7, 14, 22, and 29, with each 1% increase in %fT>MIC correlating with a 0.056 reduction in log10 cfu (95% CI: -0.092 to -0.0202 at day 7).
Detected cefpirome-resistant E.
cloacae mutants (MIC ≥ 2 μg/mL, stable after 5 subcultures in antibiotic-free broth) in only 4 rats: 2 treated with 50 mg/kg b.i.d.
(550 cfu/g and 440 cfu/g at day 7, declining to 20 cfu/g and remaining at 400 cfu/g by day 43, respectively), 1 treated with 25 mg/kg b.i.d.
(180 cfu/g at day 7, increasing to 1×103 cfu/g by day 43), and 1 treated with 12.5 mg/kg b.i.d.
(500 cfu/g at day 43).
Molecular Weight

612.66

Formula

C22H24N6O9S3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1[C@@H](NC(/C(C2=CSC(N)=N2)=N\OC)=O)[C@@]3([H])SCC(C[N+]4=CC=CC5=C4CCC5)=C(C(O)=O)N13.O=S(O)([O-])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

H2O : < 0.1 mg/mL (insoluble)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

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Purity & Documentation

Purity: 99.49%

References
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Help & FAQs
  • 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.

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Cefpirome sulfate
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