| Size | Price | Stock | Qty |
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| 2g |
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| 5g |
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| 10g | |||
| 25g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Cefazolin Sodium targets bacterial cell wall synthesis. It inhibits the transpeptidase enzyme (penicillin-binding proteins, PBPs) that cross-links peptidoglycan chains, a critical component of the bacterial cell wall. By binding to PBPs, it disrupts cell wall synthesis, leading to cell lysis and death. Cefazolin is active against many gram-positive and some gram-negative bacteria.
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| ln Vitro |
For lipopolysaccharide-stimulated C8-B4 cells, cefazolin sodium (0-300 μg/ml; 6 or 24 hours) exhibits a direct anti-inflammatory action [2]. Cell growth brought on by IL-2, IL-4, and IL-15 is inhibited when cefazolin sodium (0-400 μM) is applied for 72 hours [3]. The phosphorylation of JAK3 induced by IL-2, IL-4, IL-15, and IL-21 is inhibited by cefazolin sodium (0-400 μM; 30 minutes) treatment [3].
In vitro, Cefazolin Sodium demonstrates bactericidal activity against a wide range of gram-positive bacteria, including Staphylococcus aureus (including penicillinase-producing strains), Streptococcus pneumoniae, and Streptococcus pyogenes. It also exhibits activity against some gram-negative bacteria such as Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis. Its antibacterial activity is characterized by minimum inhibitory concentration (MIC) values against susceptible organisms. |
| ln Vivo |
Cefazolin sodium (subcutaneous injection; 300-500 mg/kg; once daily; 5 d) treatment can improve the postoperative learning and memory abilities of mice [2].
Cefazolin Sodium is administered via intravenous or intramuscular injection. It is commonly used for surgical prophylaxis to prevent infections, as well as for the treatment of skin and soft tissue infections, respiratory tract infections, and urinary tract infections. The compound achieves therapeutic concentrations in various tissues and body fluids. |
| Enzyme Assay |
The antibacterial activity of Cefazolin Sodium is assessed using standard antimicrobial susceptibility testing methods, such as broth microdilution or agar diffusion assays. The minimum inhibitory concentration (MIC) against various bacterial strains is determined by incubating bacteria with serial dilutions of the compound and observing growth inhibition. The MIC values are used to quantify the compound's antibacterial potency.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: C8-B4 Cell Tested Concentrations: 0, 50, 100, 150, 200, 250 or 300 μg/ml Incubation Duration: 6 or 24 hrs (hours) Experimental Results: Complete inhibition of IL-1β with increasing doses, but The increase in IL-6 was inhibited only at 200 μg/ml. Cell proliferation assay[3] Cell Types: PBMC and TF-1 Cell Tested Concentrations: 0, 100, 200 and 400 μM Incubation Duration: 72 hrs (hours) Experimental Results: diminished cell proliferation induced by IL-2, IL-4 and IL-15, indicating Cefazolin not only interferes with IL-15Rα but also with IL-2/IL-15Rβ and/or γc. Cell viability assay [3] Cell Types: PBMC, NK-92 and TF-1 Cell Tested Concentrations: 0, 100, 200 and 400 μM Incubation Duration: 30 minutes Experimental Results: The phosphorylation of JAK3 was diminished after cytokine treatment, which was concluded to inhibit γc Receptor signal transduction. |
| Animal Protocol |
Animal/Disease Models: 6 to 8 weeks old male CD-1 mice underwent clinical exploratory laparotomy [2]
Doses: 300-500 mg/kg Route of Administration: subcutaneous injection; 300-500 mg/kg; one time/day; 5-day Experimental Results: Surgery-induced learning and memory dysfunction is attenuated. |
| ADME/Pharmacokinetics |
Cefazolin Sodium has a molecular formula of C14H13N8NaO4S3 and a molecular weight of 476.48 g/mol. Its CAS number is 27164-46-1. It is a white to off-white crystalline powder. It is soluble in water and should be stored according to the manufacturer's instructions.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Limited information suggests that cefazolin concentrations in breast milk are low and are not expected to have adverse effects on breastfed infants. There are reports that cephalosporins occasionally disrupt the infant's gut microbiota, leading to diarrhea or thrush, but these effects have not been fully assessed. Cefazolin is safe for use by breastfeeding women. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. Cefazolin Sodium is generally well-tolerated. Common side effects include pain at the injection site, gastrointestinal disturbances, and allergic reactions. It is contraindicated in patients with a history of hypersensitivity to cephalosporins or penicillins. As with all antibiotics, it should be used under medical supervision. |
| References | |
| Additional Infomation |
Cefazolin sodium is a cephalosporin organosodium salt with side chains of [(5-methyl-1,3,4-thiadiazol-2-yl)thio]methyl and (1H-tetrazole-1-ylacetyl)amino. It contains a cefazolin (1-) domain. Cefazolin sodium is the sodium salt of cefazolin, a β-lactam antibiotic belonging to the first generation of cephalosporins with bactericidal activity. Cefazolin binds to and inactivates penicillin-binding protein (PBP) located on the inner membrane of bacterial cell walls. Inactivation of PBP interferes with the cross-linking of peptidoglycan chains, which is crucial for the strength and rigidity of bacterial cell walls, leading to weakening of the bacterial cell wall and cell lysis. Cefazolin sodium is a semi-synthetic cephalosporin analogue with broad-spectrum antibacterial activity due to its inhibition of bacterial cell wall synthesis. It can reach high serum concentrations and is rapidly excreted in the urine. See also: Cefazolin (with active fraction).
Cefazolin Sodium is a first-generation cephalosporin antibiotic used for the treatment of various bacterial infections and surgical prophylaxis. It inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins. |
| Molecular Formula |
C14H13N8NAO4S3
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|---|---|
| Molecular Weight |
476.4890
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| Exact Mass |
476.011
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| CAS # |
27164-46-1
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| Related CAS # |
Cefazolin;25953-19-9;Cefazolin sodium pentahydrate;115850-11-8
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| PubChem CID |
23675322
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| Appearance |
White to off-white solid powder
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| Melting Point |
190 °C
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| Index of Refraction |
20 ° (C=10, H2O)
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
746
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=NN=C(S1)SCC2=C(N3[C@@H]([C@@H](C3=O)NC(=O)CN4C=NN=N4)SC2)C(=O)[O-].[Na+]
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| InChi Key |
FLKYBGKDCCEQQM-WYUVZMMLSA-M
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| InChi Code |
InChI=1S/C14H14N8O4S3.Na/c1-6-17-18-14(29-6)28-4-7-3-27-12-9(11(24)22(12)10(7)13(25)26)16-8(23)2-21-5-15-19-20-21/h5,9,12H,2-4H2,1H3,(H,16,23)(H,25,26)/q+1/p-1/t9-,12-/m1./s1
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| Chemical Name |
sodium(6R,7R)-3-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfanylmethyl]-8-oxo-7-[[2-(tetrazol-1-yl)acetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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| Synonyms |
monosodium cephazolin Cefazolin sodium salt Sodium
cefazolin Sodium cephazolin Kefzol Sodium Cephazolin Sodium,
Cefazolin Sodium, Cephazolin Totacef
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ≥ 100 mg/mL (~209.87 mM)
DMSO : ~100 mg/mL (~209.87 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 100 mg/mL (209.87 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0987 mL | 10.4934 mL | 20.9868 mL | |
| 5 mM | 0.4197 mL | 2.0987 mL | 4.1974 mL | |
| 10 mM | 0.2099 mL | 1.0493 mL | 2.0987 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.
Tissue concentration of cefazolin and linezolid in sternal spongiosa in elective coronary artery bypass grafting: an in-vivo microdialysis study
CTID: null
Phase: Phase 2 Status: Ongoing
Date: 2012-05-14
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