1. Anti-infection Others
  2. Bacterial Antibiotic Drug Derivative Beta-lactamase
  3. Temocillin

Temocillin is a derivative of Ticarcillin (HY-100577) and a β-lactamase-resistant Antibiotic. Temocillin blocks water molecules from entering the active sites of Ambler class A and class C serine-dependent β-lactamases, resisting hydrolysis by these enzymes. Temocillin exhibits antibacterial activity against Enterobacteriaceae and Neisseria gonorrhoeae. Temocillin shows antagonistic effects against some isolated strains when used in combination with Ticarcillin (HY-100577) or Cefazolin (HY-B1892). Temocillin can be used in research related to sepsis, urinary tract infections, and lower respiratory tract infections.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form that retains the same biological activity.

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

Temocillin

Temocillin Chemical Structure

CAS No. : 66148-78-5

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Description

Temocillin is a derivative of Ticarcillin (HY-100577) and a β-lactamase-resistant Antibiotic. Temocillin blocks water molecules from entering the active sites of Ambler class A and class C serine-dependent β-lactamases, resisting hydrolysis by these enzymes. Temocillin exhibits antibacterial activity against Enterobacteriaceae and Neisseria gonorrhoeae. Temocillin shows antagonistic effects against some isolated strains when used in combination with Ticarcillin (HY-100577) or Cefazolin (HY-B1892). Temocillin can be used in research related to sepsis, urinary tract infections, and lower respiratory tract infections[1][2][3].

IC50 & Target

β-lactam

 

In Vitro

Temocillin exhibits potent activity against wild-type Enterobacteriaceae (MIC50 2-16 mg/L, MIC90 4-32 mg/L) and Neisseria gonorrhoeae (MIC50 0.5 mg/L, MIC90 1 mg/L), but no activity against Gram-positive cocci, Pseudomonas aeruginosa, or Acinetobacter spp., and acts as a bactericidal agent against Enterobacteriaceae with MBC values equivalent to or twofold higher than MIC values[1].
Temocillin is highly active against ESBL-, CTX-M-, non-CTX-M ESBL-, dAmpC-, and KPC-producing Enterobacteriaceae (≤99% susceptible at MIC50 ≤32 mg/L), but has minimal activity against OXA-48- and VIM/NDM/IMP-producing Enterobacteriaceae[1].
Temocillin shows a mild inoculum effect against β-lactamase-negative or ESBL/KPC-producing Enterobacteriaceae, but a marked inoculum effect (8- to 16-fold MBC increase) against chromosomic AmpC β-lactamase-producing Enterobacteriaceae[1].
Temocillin shows in vitro activity against susceptible and KPC-producing E. coli CFT073 strains with MIC50-like MIC values of 8, 16, and 32 mg/L, respectively, but has minimal activity against OXA-48-producing E. coli CFT073 with an MIC of 256 mg/L[2].\n\nWait, correction: The original text uses "MICs" and "MIC" which are potency indicators, so they should be bolded with subscript if applicable, but since it's just MIC (minimum inhibitory concentration), which is a potency indicator, we format it as MIC. Also, fix the earlier error where I incorrectly added MIC50 which wasn't in the original. Here's the correct formatted text:\n\nTemocillin shows in vitro activity against susceptible and KPC-producing E. coli CFT073 strains with MICs of 8, 16, and 32 mg/L, respectively, but has minimal activity against OXA-48-producing E. coli CFT073 with an MIC of 256 mg/L[2].
Temocillin (18-24 h) potently inhibits most β-lactamase-producing Gram-negative Enterobacteriaceae, Haemophilus influenzae, and Neisseria gonorrhoeae with MIC90 values ≤16 μg/mL or ≤1 μg/mL, respectively, but is ineffective against Pseudomonas spp., Acinetobacter spp., and all tested Gram-positive bacteria[3].
Temocillin (0.1 mM; 10-30 min) potently inhibits Escherichia coli TEM-1, Enterobacter cloacae P99, and Morganella morganii β-lactamases, completely blocking cephaloridine hydrolysis by TEM-1 and Morganella sp. enzymes[3].
Temocillin (30 μg disk; variable dilution) exhibits antagonistic activity with ticarcillin against some Pseudomonas aeruginosa isolates and with cefazolin against multiple bacterial species, but does not antagonize gentamicin or tobramycin[3].

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

Parmacokinetics
Species Dose Route Serum Concentration
Mice[2] 200 mg/kg s.c. 96.2 (30 min) mg/L
Molecular Weight

414.45

Formula

C16H18N2O7S2

CAS No.
SMILES

OC(C(C1=CSC=C1)C(N[C@]2([C@]3([H])N([C@H](C(C)(S3)C)C(O)=O)C2=O)OC)=O)=O

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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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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Temocillin
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