| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Primary target is penicillin-binding proteins (PBPs) in the bacterial cell wall. Cefcapene acylates PBPs, blocking peptidoglycan cross-linking and causing bactericidal activity. The prodrug requires esterase hydrolysis for activation. Selectivity for bacterial versus mammalian cells is inherent.
|
|---|---|
| ln Vitro |
Active cefcapene shows broad-spectrum antibacterial activity. MIC values are determined by broth microdilution against clinical isolates. The prodrug is inactive in vitro until hydrolyzed. Activity is bactericidal, as confirmed by time-kill assays.
|
| ln Vivo |
Cefcapene pivoxil is orally active and used clinically for bacterial infections. It achieves therapeutic plasma concentrations after oral administration. Efficacy is established in clinical settings for skin, respiratory, and urinary tract infections.
|
| Enzyme Assay |
For PBP binding, isolated bacterial membranes or purified PBPs are incubated with a fluorescent or radiolabeled penicillin in the presence of cefcapene, and competition is measured. IC50 values are derived from dose-response curves.
|
| Cell Assay |
Bacterial cultures are grown in standardized medium, and MIC is determined by broth microdilution. Time-kill assays assess bactericidal activity. β-Lactamase stability is assessed with nitrocefin. Mammalian cytotoxicity is measured in parallel.
|
| Animal Protocol |
Mice or rats are infected with bacterial strains and treated orally with cefcapene pivoxil at defined doses. Survival, tissue bacterial burden, and plasma concentrations are monitored. Pharmacokinetic parameters are derived from plasma sampling.
|
| References | |
| Additional Infomation |
Cefcapene pivoxil hydrochloride hydrate is the hydrated hydrochloride form of Cefcapene pitavaate, a prodrug belonging to the third-generation cephalosporins with antibacterial activity. Upon oral administration of Cefcapene pivoxil hydrochloride hydrate, the ester bond breaks, releasing the active ingredient Cefcapene.
|
| Molecular Formula |
C23H29N5O8S2
|
|---|---|
| Molecular Weight |
567.63506
|
| Exact Mass |
567.145
|
| CAS # |
105889-45-0
|
| Related CAS # |
Cefcapene pivoxil hydrochloride;147816-23-7;Cefcapene pivoxil hydrochloride hydrate;147816-24-8
|
| PubChem CID |
5282437
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
888.4±65.0 °C at 760 mmHg
|
| Melting Point |
158-164ºC
|
| Flash Point |
491.1±34.3 °C
|
| Vapour Pressure |
0.0±0.3 mmHg at 25°C
|
| Index of Refraction |
1.639
|
| LogP |
1.1
|
| tPSA |
246.78
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
13
|
| Rotatable Bond Count |
13
|
| Heavy Atom Count |
40
|
| Complexity |
1060
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
NC(OCC1CS[C@@H]2[C@@H](C(=O)N2C=1C(OCOC(C(C)(C)C)=O)=O)NC(/C(/C1=CSC(N)=N1)=C\CC)=O)=O
|
| InChi Key |
LUXIJPQYUCFVAL-XRLCNELCSA-N
|
| InChi Code |
InChI=1S/C23H29N5O8S2.ClH.H2O/c1-5-6-12(13-9-38-21(24)26-13)16(29)27-14-17(30)28-15(11(7-34-22(25)33)8-37-18(14)28)19(31)35-10-36-20(32)23(2,3)4;;/h6,9,14,18H,5,7-8,10H2,1-4H3,(H2,24,26)(H2,25,33)(H,27,29);1H;1H2/b12-6-;;/t14-,18-;;/m1../s1
|
| Chemical Name |
2,2-dimethylpropanoyloxymethyl (6R,7R)-7-[[(Z)-2-(2-amino-1,3-thiazol-4-yl)pent-2-enoyl]amino]-3-(carbamoyloxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate;hydrate;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 1.7617 mL | 8.8084 mL | 17.6168 mL | |
| 5 mM | 0.3523 mL | 1.7617 mL | 3.5234 mL | |
| 10 mM | 0.1762 mL | 0.8808 mL | 1.7617 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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