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Cefoperazone

Catalog No.
A8392
Third-generation cephalosporin antibiotic
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$66.00
In stock
50mg
$55.00
In stock
1g
$77.00
In stock
5g
$110.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Cefoperazone is a cephalosporin antibiotic which inhibits rMrp2-mediated [3H]E217βG uptake with an IC50 of 199 μM [1].

The inhibition profile for cefoperazone was biphasic with IC50, high and IC50, low values of 6.66 ± 3.23 μM and 3.88 ± 1.32 mM, respectively, indicating that cefoperazone may inhibit two binding sites that mediated [3H]E217βG transport [1]. Cefoperazone is a sterile, broad-spectrum, semisynthetic, parenteral cephalosporin antibiotic for intravenous or intramuscular administration. After intravenous administration of 2 g cefoperazone, levels in serum ranged from 202 μg/mL to 375 μg/mL depending on the period of drug administration. After intramuscular injection of 2 g of cefoperazone, the mean peak serum level was111 μg/mL at 1.5 hours. At 12 hours after dosing, mean serum levels were still 2 to 4 μg/mL.Cefoperazone is 90% bound to serum proteins.The apparent volume of distribution was 10 to 13L. The half-life of the drug varied from 1.6 to 2.4 hours, and the serum clearance was between 75 and 96 ml/min [2].

References:
[1].  Kato Y1,Takahara S,Kato S,Kubo Y,Sai Y,Tamai I,Yabuuchi H,Tsuji A. Involvement of multidrug resistance-associated protein 2 (Abcc2) in molecular weight-dependent biliary excretion of beta-lactam antibiotics.Drug Metab Dispos.2008 Jun;36(6):1088-96. doi: 10.1124/dmd.107.019125. Epub 2008 Mar 13.
[2].  Craig WA,Gerber AU. Pharmacokinetics of cefoperazone: a review. Drugs.1981;22Suppl 1:35-45.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt645.66
Cas No.62893-19-0
FormulaC25H27N9O8S2
Solubility≥64.6 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name(6R,7R)-7-[[(2R)-2-[(4-ethyl-2,3-dioxopiperazine-1-carbonyl)amino]-2-(4-hydroxyphenyl)acetyl]amino]-3-[(1-methyltetrazol-5-yl)sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
SDFDownload SDF
Canonical SMILESCCN1CCN(C(=O)C1=O)C(=O)NC(C2=CC=C(C=C2)O)C(=O)NC3C4N(C3=O)C(=C(CS4)CSC5=NN=NN5C)C(=O)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Animal experiment [1]:

Animal models

Male Sprague-Dawley rats (SDRs)

Dosage form

20 mg/kg(i.v.)

Application

Compared with SDRs, the disappearance of cefoperazone plasma in EHBRs was delayed, and the CLtotal of cefoperazone in EHBRs was significantly lower and the average residence time was longer.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Kato Y, Takahara S, Kato S, Kubo Y, Sai Y, Tamai I, Yabuuchi H, Tsuji A.Involvement of multidrug resistance-associated protein 2 (Abcc2) in molecular weight-dependent biliary excretion of beta-lactam antibiotics. Drug Metab Dispos. 2008 Jun;36(6):1088-96. doi: 10.1124/dmd.107.019125. Epub 2008 Mar 13. PubMed PMID: 18339814.

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