| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
- Ceftezole sodium inhibits α-glucosidase (a key enzyme in carbohydrate digestion), with an IC50 of 2.3 μM against yeast α-glucosidase and 3.1 μM against rat intestinal mucosal α-glucosidase[1]
- Ceftezole sodium acts as a cephem antibiotic by targeting bacterial penicillin-binding proteins (PBPs) to inhibit bacterial cell wall synthesis[1,2] |
|---|---|
| ln Vitro |
- α-Glucosidase inhibitory activity: Ceftezole sodium inhibited α-glucosidase in a concentration-dependent manner. At 10 μM, it reduced yeast α-glucosidase activity by 85% and rat intestinal mucosal α-glucosidase activity by 78% (using p-nitrophenyl-α-D-glucopyranoside (pNPG) as the substrate). At 5 μM, it reduced sucrose hydrolysis by 62% and maltose hydrolysis by 55% compared to the control group[1]
- Antibacterial activity: Ceftezole sodium exhibited in vitro antibacterial activity against Gram-positive bacteria (e.g., Staphylococcus aureus , Streptococcus pyogenes ) with minimum inhibitory concentrations (MICs) ranging from 0.25 to 2 μg/mL[1] |
| ln Vivo |
- Antidiabetic activity in STZ-induced diabetic mice: Male ICR mice with streptozotocin (STZ)-induced diabetes (fasting blood glucose > 300 mg/dL) were treated with Ceftezole sodium (100 mg/kg, 200 mg/kg, intraperitoneal injection) once daily for 21 days. The 200 mg/kg dose decreased postprandial blood glucose (2 hours after sucrose loading) by 45% and glycated hemoglobin (HbA1c) levels by 32% compared to the diabetic control group[1]
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| Enzyme Assay |
- α-Glucosidase activity assay: Yeast α-glucosidase or rat intestinal mucosal α-glucosidase was mixed with Ceftezole sodium (0.1–20 μM) in pH 6.8 buffer and pre-incubated at 37°C for 10 minutes. The reaction was initiated by adding pNPG (final concentration 5 mM) and incubated for 30 minutes. The reaction was terminated with 0.1 M Na₂CO₃, and absorbance was measured at 405 nm to quantify p-nitrophenol release. Inhibition rate was calculated as [(control absorbance - drug group absorbance) / control absorbance] × 100%[1]
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| Animal Protocol |
- STZ-induced diabetic mouse model: Male ICR mice (6–8 weeks old) were injected intraperitoneally with STZ (150 mg/kg, dissolved in citrate buffer, pH 4.5) to induce diabetes. After 7 days, mice with fasting blood glucose > 300 mg/dL were divided into 3 groups (n=8/group): diabetic control (saline, IP), Ceftezole sodium 100 mg/kg (IP), Ceftezole sodium 200 mg/kg (IP). Drugs were administered daily for 21 days. Fasting blood glucose was measured weekly; postprandial glucose was tested 2 hours after oral sucrose (2 g/kg) on day 21; HbA1c was analyzed at the end[1]
- Pharmacokinetic animal model: Male Wistar rats (250–300 g) and New Zealand rabbits (2–2.5 kg) received Ceftezole sodium (dissolved in saline) via intravenous (IV, 20 mg/kg) or intramuscular (IM, 20 mg/kg) injection. Blood samples were collected at 0.25–8 hours post-administration; tissues (liver, kidney, lung, muscle) were sampled at 1 hour post-IV. Urine and feces were collected for 24 hours to determine excretion rates[2] |
| ADME/Pharmacokinetics |
Absorption: Ceftezole sodium is rapidly absorbed after intramuscular injection. After intramuscular injection of 20 mg/kg in rats, the peak plasma concentration (Cmax) was 18 μg/mL, and the time to peak concentration was 0.5 hours (Tmax); after intramuscular injection of 20 mg/kg in rabbits, the peak plasma concentration (Cmax) was 22 μg/mL, and the time to peak concentration was 0.5 hours [2]
- Distribution: After intravenous injection of 20 mg/kg Ceftezole sodium in rats, the distribution was extensive: at 1 hour, the blood drug concentrations in the liver (12 μg/g), kidney (25 μg/g), lung (8 μg/g), and muscle (5 μg/g) were all high. The plasma protein binding rate in both animals was 10%–15% [2] - Metabolism and excretion: Ceftezole sodium is metabolized very little. Within 24 hours, more than 80% of the dose was excreted unchanged in the urine (rat: 85%, rabbit: 82%); fecal excretion was <5%. The plasma elimination half-life (t1/2) was 1.2 hours (rat) and 1.5 hours (rabbit), respectively.[2] |
| Toxicity/Toxicokinetics |
In vivo toxicity: No acute toxicity was observed in rats and rabbits at intravenous/intramuscular doses up to 200 mg/kg. Serum ALT, AST, BUN and creatinine levels remained normal [2]
- In vitro cytotoxicity: Ceftezole sodium (concentrations up to 100 μM) showed no significant toxicity to normal rat intestinal epithelial cells (cell survival rate > 90% after 24 hours) [1] |
| References | |
| Additional Infomation |
Ceftezole sodium is an N-acyl amino acid.
Ceftezole sodium is the sodium salt form of Ceftezole, a semi-synthetic first-generation cephalosporin with antibacterial activity. - Ceftezole sodium is a first-generation cephalosporin antibiotic derived from cephalosporin C, used clinically to treat Gram-positive bacterial infections[2]. - Its antidiabetic activity is independent of its antibacterial action, delaying carbohydrate absorption and reducing postprandial hyperglycemia by inhibiting α-glucosidase[1]. |
| Molecular Formula |
C13H11N8NAO4S3
|
|---|---|
| Molecular Weight |
462.4624
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| Exact Mass |
461.996
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| CAS # |
41136-22-5
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| Related CAS # |
Ceftezole;26973-24-0
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| PubChem CID |
23688977
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| Appearance |
White to off-white solid powder
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| Density |
2.09 g/cm3
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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 |
29
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| Complexity |
716
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1C(=C(N2[C@H](S1)[C@@H](C2=O)NC(=O)CN3C=NN=N3)C(=O)[O-])CSC4=NN=CS4.[Na+]
|
| InChi Key |
UGUMHWUOXWFPFH-JHQAJZDGSA-M
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| InChi Code |
InChI=1S/C13H12N8O4S3.Na/c22-7(1-20-4-14-18-19-20)16-8-10(23)21-9(12(24)25)6(2-26-11(8)21)3-27-13-17-15-5-28-13;/h4-5,8,11H,1-3H2,(H,16,22)(H,24,25);/q;+1/p-1/t8-,11-;/m1./s1
|
| Chemical Name |
sodium;(6R,7R)-8-oxo-7-[[2-(tetrazol-1-yl)acetyl]amino]-3-(1,3,4-thiadiazol-2-ylsulfanylmethyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
|
| 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 : ~250 mg/mL (~540.59 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (216.23 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1623 mL | 10.8117 mL | 21.6235 mL | |
| 5 mM | 0.4325 mL | 2.1623 mL | 4.3247 mL | |
| 10 mM | 0.2162 mL | 1.0812 mL | 2.1623 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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