| Size | Price | Stock | Qty |
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| 100mg |
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| 1g | |||
| Other Sizes |
| Targets |
Cephradine monohydrate targets bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), which are enzymes involved in the cross-linking of peptidoglycan chains. By inhibiting transpeptidase activity, it prevents the formation of a stable cell wall, leading to bacterial cell lysis and death. It also blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK (T-LAK cell-originated protein kinase).
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| ln Vitro |
Cefradine (0~8 μg/mL; 12 hours) can quickly increase bacterial viability at pH 7.4 and pH 5.5 when the antibiotic concentration is less than the MIC (minimum inhibitory concentration) of 0.70 μg/mL [4].
In vitro, Cephradine monohydrate exhibits broad-spectrum antibacterial activity against both Gram-positive and Gram-negative pathogens. It is effective against most penicillinase-producing organisms that are resistant to penicillin G, penicillin V, and ampicillin. Its mechanism of action involves inhibition of bacterial cell wall synthesis, leading to bactericidal effects. Minimum inhibitory concentration (MIC) values vary depending on the bacterial strain. |
| ln Vivo |
In abscesses, cefradine (25 mg/kg; subcutaneous; 11 days) lowers bacterial numbers and density [4].
In vivo, Cephradine monohydrate is an orally active cephalosporin used for the treatment of various bacterial infections. It has been used in the research and treatment of genitourinary, gastrointestinal, and respiratory tract infections, as well as infections of the skin and soft tissues. It is also used to treat urinary tract infections, skin infections, chest and throat infections, ear infections, and sinusitis. |
| Enzyme Assay |
In vitro antibacterial susceptibility testing for Cephradine monohydrate is conducted using broth microdilution or disk diffusion methods following Clinical and Laboratory Standards Institute (CLSI) guidelines. Bacterial strains are cultured in appropriate media and incubated with serial dilutions of the antibiotic. The minimum inhibitory concentration (MIC) is determined as the lowest concentration that inhibits visible bacterial growth after 18-24 hours of incubation.
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| Cell Assay |
Cephradine monohydrate is not typically used in mammalian cell-based assays, as it targets bacterial cells. However, cytotoxicity assays may be conducted in mammalian cell lines to assess potential toxicity. TOPK inhibition assays may be performed using relevant cell lines to study the anti-inflammatory effects of the compound.
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| Animal Protocol |
Animal/Disease Models: Non-diabetic mice
Doses: 25 mg/kg Route of Administration: Sc; 11 days Experimental Results: diminished bacterial density and counts in abscesses. Cephradine monohydrate is used in animal models of infection to evaluate its in vivo efficacy. Rodent models of urinary tract infection, pneumonia, or skin and soft tissue infection are commonly used. The antibiotic is administered orally or parenterally. Endpoints include survival, bacterial load in tissues, and histopathological evaluation of infected organs. |
| ADME/Pharmacokinetics |
Cephradine monohydrate is an orally active cephalosporin with good oral bioavailability. It has a molecular weight of 367.42 and a molecular formula of C₁₆H₂₁N₃O₅S. It is absorbed from the gastrointestinal tract and distributed to various tissues. It is excreted primarily in the urine. Its half-life is approximately 1-2 hours in patients with normal renal function.
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| Toxicity/Toxicokinetics |
Cephradine monohydrate is generally well-tolerated. Common side effects include gastrointestinal disturbances such as diarrhea, nausea, and vomiting. Allergic reactions may occur in patients with hypersensitivity to penicillins or cephalosporins. It should be used with caution in patients with renal impairment.
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| References |
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| Additional Infomation |
Cephradine monohydrate is the monohydrate form of Cephradine, a first-generation β-lactam cephalosporin antibiotic with bactericidal activity. Cephradine monohydrate binds to and inactivates penicillin-binding protein (PBP) located on the inner membrane of the bacterial cell wall. PBP is involved in the final stages of bacterial cell wall assembly and cell wall remodeling during cell division. Inactivation of PBP interferes with the cross-linking of peptidoglycan chains, which is crucial for maintaining the strength and rigidity of the bacterial cell wall. This leads to weakening of the bacterial cell wall, ultimately resulting in cell lysis.
Cephradine monohydrate is a first-generation cephalosporin antibiotic with broad-spectrum activity against Gram-positive and Gram-negative pathogens. It is orally active and used to treat genitourinary, gastrointestinal, respiratory, skin, and soft tissue infections. It also blocks solar-ultraviolet induced skin inflammation via TOPK inhibition. It is an approved antibiotic. |
| Molecular Formula |
C16H19N3O4S.2[H2O]
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|---|---|
| Molecular Weight |
385.43532
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| Exact Mass |
367.12
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| CAS # |
75975-70-1
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| Related CAS # |
Cephradine;38821-53-3
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| PubChem CID |
21124775
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| Appearance |
Typically exists as solid at room temperature
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| Melting Point |
140-142° (dec)
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
697
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=C(N2C(C(C2=O)NC(=O)C(C3=CCC=CC3)N)SC1)C(=O)O.O
|
| InChi Key |
VHNPSPMQGXQSET-CYJZLJNKSA-N
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| InChi Code |
InChI=1S/C16H19N3O4S.H2O/c1-8-7-24-15-11(14(21)19(15)12(8)16(22)23)18-13(20)10(17)9-5-3-2-4-6-9;/h2-3,6,10-11,15H,4-5,7,17H2,1H3,(H,18,20)(H,22,23);1H2/t10-,11-,15-;/m1./s1
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| Chemical Name |
(6R,7R)-7-[[(2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetyl]amino]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid;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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5944 mL | 12.9722 mL | 25.9444 mL | |
| 5 mM | 0.5189 mL | 2.5944 mL | 5.1889 mL | |
| 10 mM | 0.2594 mL | 1.2972 mL | 2.5944 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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