| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Cephaloridine targets penicillin-binding proteins (PBPs) located in the bacterial cell wall, particularly transpeptidases involved in the final stage of peptidoglycan synthesis. By binding to these enzymes, cephaloridine inhibits the cross-linking of peptidoglycan chains, leading to a weakened cell wall that is susceptible to osmotic lysis. Its antibacterial spectrum includes both Gram-positive and some Gram-negative bacteria. The compound's primary targets are bacterial PBPs, which are essential for cell wall integrity and bacterial survival.
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| ln Vitro |
At a minimum inhibitory concentration (MIC) of 0.05–1 μg/mL, cephaloridine hydrate can inhibit both penicillin-sensitive and penicillin-resistant strains of Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Corynebacterium diphtheriae, and other bacteria[1].
Cephaloridine hydrate demonstrates potent in vitro antibacterial activity against a wide range of bacterial pathogens. At minimum inhibitory concentrations (MIC) of 0.05-1 microg/mL, cephaloridine hydrate inhibits both penicillin-sensitive and penicillin-resistant strains of Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Corynebacterium diphtheriae, and other susceptible organisms. Its broad-spectrum activity makes it effective against many Gram-positive bacteria and some Gram-negative bacteria. The compound's in vitro activity is typically assessed using standard broth microdilution or agar dilution methods to determine MIC values. |
| ln Vivo |
In rabbits and monkeys, cephaloridine hydrate (50–500 mg/kg; intramuscular injection) shows dose-related nephrotoxicity [2].
In vivo activity of cephaloridine hydrate has been demonstrated in animal models of bacterial infection, though its clinical use has been limited by nephrotoxicity. The compound exhibits antibacterial efficacy against susceptible pathogens in vivo, with activity correlating with in vitro MIC values. Its bactericidal activity is time-dependent, requiring sustained concentrations above the MIC for optimal efficacy. However, the compound's dose-related nephrotoxicity has limited its therapeutic application, and it is primarily used in research settings to study antibiotic mechanisms and toxicity. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for cephaloridine hydrate involve assessing its binding affinity to penicillin-binding proteins (PBPs). The assay typically uses isolated bacterial membranes or purified PBPs and radiolabeled penicillin (e.g., [14C]-penicillin G) in a competitive binding format. The compound is incubated with the PBP preparation, and bound radioactivity is quantified after filtration or precipitation. The concentration required to displace 50% of the labeled penicillin (IC₅0) is determined. Alternatively, the compound's inhibition of transpeptidase activity can be measured using a synthetic peptide substrate, with enzyme activity quantified by HPLC or colorimetric detection.
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| Cell Assay |
Cellular assays for cephaloridine hydrate are conducted using bacterial cultures to determine its antibacterial activity. Standard broth microdilution or agar dilution methods are used to determine minimum inhibitory concentrations (MIC) against various bacterial strains. Bacteria are cultured in appropriate media at 37degC for 18-24 hours in the presence of serial dilutions of the compound. The MIC is defined as the lowest concentration that inhibits visible bacterial growth. Time-kill assays are performed to determine the bactericidal kinetics, and post-antibiotic effects are assessed by measuring the time required for bacterial regrowth after removal of the antibiotic.
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| Animal Protocol |
In vivo animal studies with cephaloridine hydrate have been conducted to evaluate its antibacterial efficacy and toxicity. Murine models of systemic infection (e.g., peritoneal or intravenous injection of bacteria) are commonly used. Infected animals are treated with the compound via subcutaneous or intramuscular injection at various doses, and survival rates or bacterial counts in target organs are measured. Nephrotoxicity studies involve administering varying doses of the compound to rats or other animals and monitoring renal function parameters such as serum creatinine, blood urea nitrogen, and histopathological examination of kidney tissues. These studies have demonstrated the compound's dose-related nephrotoxic potential.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of cephaloridine hydrate have been characterized in preclinical and clinical studies. The compound is administered parenterally due to poor oral absorption. It is distributed widely in body tissues and fluids, including the kidneys, where it achieves high concentrations. Cephaloridine is primarily excreted unchanged by the kidneys via glomerular filtration and tubular secretion, with a relatively short half-life in patients with normal renal function. Its molecular weight is 433.50 g/mol. The compound's nephrotoxicity is related to its accumulation in renal proximal tubular cells, where it undergoes intracellular accumulation and causes cellular damage.
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| Toxicity/Toxicokinetics |
Toxicological data for cephaloridine hydrate demonstrate dose-related nephrotoxicity, which is the primary adverse effect limiting its clinical use. The compound accumulates in renal proximal tubular cells, leading to cellular damage and dysfunction. Nephrotoxicity is manifested by increased serum creatinine, decreased creatinine clearance, and histopathological changes including tubular necrosis. The compound may also cause hypersensitivity reactions and gastrointestinal disturbances. In preclinical toxicology studies, the compound's nephrotoxic effects are dose-dependent and are exacerbated by dehydration and concurrent use of other nephrotoxic agents.
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| References |
[1]. P. W. Muggleton, et al. Laboratory Evaluation of a New Antibiotic-Cephaloridine (Ceporin). Br Med J. 1964 Nov 14;2(5419):1234-7.
[2]. Perkins RL, et al. Cephaloridine and cephalothin: comparative studies of potential nephrotoxicity. J Lab Clin Med. 1968 Jan;71(1):75-84. |
| Additional Infomation |
Cephaloridine hydrate is a first-generation cephalosporin antibiotic with broad-spectrum antibacterial activity. It is effective against both penicillin-sensitive and penicillin-resistant strains of various bacteria, with MIC values of 0.05-1 microg/mL. The compound is a derivative of cephalosporin C and is used in research to study transpeptidase expression, binding, and inhibition on bacterial cell wall mucopeptide synthesis. Its clinical use has been limited by dose-related nephrotoxicity. The compound is not widely used clinically but remains a valuable research tool for studying antibiotic mechanisms and toxicity.
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| Molecular Formula |
C19H19N3O5S2
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| Molecular Weight |
433.50
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| Exact Mass |
433.077
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| CAS # |
102039-86-1
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| Related CAS # |
Cephaloridine;50-59-9
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| PubChem CID |
51063108
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
687
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1C(=C(N2C(S1)C(C2=O)NC(=O)CC3=CC=CS3)C(=O)[O-])C[N+]4=CC=CC=C4.O
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| InChi Key |
KZYZSCXFERELNV-KQKCUOLZSA-N
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| InChi Code |
InChI=1S/C19H17N3O4S2.H2O/c23-14(9-13-5-4-8-27-13)20-15-17(24)22-16(19(25)26)12(11-28-18(15)22)10-21-6-2-1-3-7-21;/h1-8,15,18H,9-11H2,(H-,20,23,25,26);1H2/t15-,18-;/m1./s1
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| Chemical Name |
(6R,7R)-8-oxo-3-(pyridin-1-ium-1-ylmethyl)-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate;hydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : 125 mg/mL (288.35 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3068 mL | 11.5340 mL | 23.0681 mL | |
| 5 mM | 0.4614 mL | 2.3068 mL | 4.6136 mL | |
| 10 mM | 0.2307 mL | 1.1534 mL | 2.3068 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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