| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Aspoxicillin targets penicillin-binding proteins (PBPs) in the bacterial cell wall. By binding to PBPs, Aspoxicillin inhibits the transpeptidase activity that cross-links peptidoglycan chains, a critical step in bacterial cell wall synthesis. This inhibition leads to the weakening of the cell wall, osmotic instability, and ultimately bacterial cell lysis and death. Aspoxicillin's spectrum of activity includes both Gram-positive and Gram-negative bacteria, although its activity against β-lactamase-producing organisms is limited.
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| ln Vitro |
Aspoxicillin is a semi-synthetic derivative of penicillin [2]. In vitro, Aspoxicillin has a 1.7-hour post-antibiotic effect (PAE) on Staphylococcus aureus Smith.
In vitro, Aspoxicillin has been shown to possess antibacterial activity against a variety of bacterial pathogens, including Streptococcus pneumoniae, Staphylococcus aureus, Escherichia coli, and Haemophilus influenzae. The minimum inhibitory concentration (MIC) of Aspoxicillin against these organisms ranges from 0.1 to 10 µg/mL. The compound's activity is comparable to that of ampicillin and amoxicillin, with enhanced stability against certain β-lactamases. Aspoxicillin is bactericidal, with time-kill studies demonstrating rapid bacterial killing. |
| ln Vivo |
For 5.2 hours, apocillin produced PAE against S. aureus Smith in vivo in a thigh infection model in neutropenic mice [2].
After intravenously injecting hydroxychloroquine (5 mg/kg) into BALB/c mice, the amount of chlorotoquine (desethylhydroxychloroquine) in the mice's blood and tissues was measured. Tissue-to-blood concentration ratio (Kp) ≥1 signifies tissue accumulation of chlorotoquine. From high to low, the following tissues had the highest chlorotoquine Kp ratios: liver (114.3), kidney (24.4), spleen (19.3), lung (16.5), heart (5.5) [3].
In vivo, Aspoxicillin has been shown to be effective in the treatment of various bacterial infections in animal models. The compound's efficacy has been demonstrated in models of respiratory tract infection, urinary tract infection, and septicemia. In clinical studies, Aspoxicillin has been shown to be effective in the treatment of patients with respiratory tract infections, urinary tract infections, and other bacterial infections. The compound's safety and efficacy have been established through clinical use. |
| Enzyme Assay |
In vitro susceptibility testing for Aspoxicillin is performed using the broth microdilution or disk diffusion method according to CLSI guidelines. The minimum inhibitory concentration (MIC) is determined by incubating bacteria with serial dilutions of the compound in Mueller-Hinton broth. The MIC is defined as the lowest concentration of the compound that inhibits visible bacterial growth after 18-24 hours of incubation. The zone of inhibition is measured for disk diffusion testing.
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| Cell Assay |
In vitro cellular experiments for Aspoxicillin are not typically performed, as the compound is an antibacterial agent that targets bacterial cell wall synthesis. However, its effects on bacterial morphology and viability can be assessed using microscopy and flow cytometry. The compound's ability to induce bacterial cell lysis can be assessed by measuring the release of intracellular contents, such as ATP or cytoplasmic enzymes.
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| Animal Protocol |
In vivo animal studies for Aspoxicillin are conducted using mouse or rat models of bacterial infection. Animals are infected with a pathogenic bacterial strain and then treated with Aspoxicillin via intravenous or intramuscular injection. The efficacy of the treatment is evaluated by monitoring survival, bacterial burden in tissues, and clinical signs of infection. The compound's safety and tolerability are also assessed.
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| ADME/Pharmacokinetics |
Aspoxicillin exhibits favorable pharmacokinetic properties following parenteral administration. The compound is rapidly distributed to various tissues and achieves therapeutic concentrations in the blood, lungs, and urine. It has a half-life of approximately 1-2 hours, requiring multiple daily doses. Aspoxicillin is primarily excreted unchanged in the urine, and dose adjustment may be necessary in patients with renal impairment.
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| Toxicity/Toxicokinetics |
The toxicity profile of Aspoxicillin is similar to that of other penicillins. Common adverse effects include gastrointestinal disturbances, such as nausea, vomiting, and diarrhea. Allergic reactions, including rash, urticaria, and anaphylaxis, can occur in penicillin-sensitive patients. The compound's safety in humans has been established through its clinical use. Aspoxicillin is generally well-tolerated, with a favorable safety profile.
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| References |
[1]. Yoshimura H, et al. Comparative in vitro activity of 16 antimicrobial agents against Actinobacillus pleuropneumoniae. Vet Res Commun. 2002 Jan;26(1):11-9.
[2]. Oshida T, et al. Activity of sub-minimal inhibitory concentrations of aspoxicillin in prolonging the postantibiotic effect against Staphylococcus aureus. J Antimicrob Chemother. 1990 Jul;26(1):29-38. |
| Additional Infomation |
Aspirin is a peptide antibiotic. It is a broad-spectrum semi-synthetic penicillin derivative with antibacterial activity. Aspirin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of bacterial cell walls. This inactivation of PBPs interferes with the cross-linking of peptidoglycan chains, which is crucial for maintaining the strength and rigidity of bacterial cell walls. This disrupts bacterial cell wall synthesis, leading to reduced cell wall strength and ultimately cell lysis.
Aspoxicillin is a semisynthetic penicillin antibiotic used for the treatment of various bacterial infections, including respiratory tract infections, urinary tract infections, and septicemia. It is a broad-spectrum antibiotic with activity against both Gram-positive and Gram-negative bacteria. Aspoxicillin's mechanism of action involves the inhibition of penicillin-binding proteins and the disruption of bacterial cell wall synthesis. Its clinical efficacy and safety have been established through extensive use in clinical practice. |
| Molecular Formula |
C21H27N5O7S
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|---|---|
| Molecular Weight |
493.53338
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| Exact Mass |
493.163
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| Elemental Analysis |
C, 51.11; H, 5.51; N, 14.19; O, 22.69; S, 6.50
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| CAS # |
63358-49-6
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| Related CAS # |
63358-49-6;
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| PubChem CID |
71961
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| Appearance |
Solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
985.1±65.0 °C at 760 mmHg
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| Melting Point |
195-198° (dec)
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| Flash Point |
549.5±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.672
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| LogP |
-0.53
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
34
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| Complexity |
861
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC1([C@@H](N2C([C@@H](N(C([C@H](NC)CC(N)=O)=O)[C@@H](C(N)=O)C3=CC=C(O)C=C3)[C@H]2S1)=O)C(O)=O)C
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| InChi Key |
BHELIUBJHYAEDK-OAIUPTLZSA-N
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| InChi Code |
InChI=1S/C21H27N5O7S/c1-21(2)15(20(32)33)26-18(31)14(19(26)34-21)25-17(30)13(9-4-6-10(27)7-5-9)24-16(29)11(22)8-12(28)23-3/h4-7,11,13-15,19,27H,8,22H2,1-3H3,(H,23,28)(H,24,29)(H,25,30)(H,32,33)/t11-,13-,14-,15+,19-/m1/s1
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| Chemical Name |
(2S,5R,6R)-6-[[(2R)-2-[[(2R)-2-amino-4-(methylamino)-4-oxobutanoyl]amino]-2-(4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
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| Synonyms |
Aspoxicillin; TA 058; TA058; TA-058
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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) |
H2O : ~25 mg/mL (~50.66 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 12.5 mg/mL (25.33 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 | 2.0262 mL | 10.1311 mL | 20.2622 mL | |
| 5 mM | 0.4052 mL | 2.0262 mL | 4.0524 mL | |
| 10 mM | 0.2026 mL | 1.0131 mL | 2.0262 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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