| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g |
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| 2g | |||
| 5g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
β-lactam
Penicillin-binding proteins (PBPs) [2] |
|---|---|
| ln Vitro |
At ATCC 25923 and E19977, dicloxacillin displays EC50 values of 0.06 and 0.50 mg/L, respectively. In ATCC 25923 and E19977, dicloxacillin displays minimum inhibitory concentrations (MIC) of 0.125 and 0.5 mg/L at pH 7.4 respectively[3].
The study evaluated the in vitro activity of dicloxacillin sodium alone and in combination against 26 oxacillin and amikacin-resistant nosocomial Staphylococcus spp. isolates (including S. aureus and coagulase-negative staphylococci). [2] When tested alone, dicloxacillin sodium showed resistance in 88.44% (23/26) of the isolates. [2] The combination of dicloxacillin sodium with amikacin was evaluated using the checkerboard synergy test. This combination showed a synergistic effect (FIC index ≤ 0.5) against 34.6% (9/26) of the isolates and a partially synergistic effect (FIC > 0.5 but < 1) against 50% (13/26) of the isolates. For the remaining 15.4% (4/26) of isolates, the effect was additive (FIC = 1). No antagonistic effects were observed. [2] For nearly half of the isolates, the mean concentrations of dicloxacillin sodium at which the FIC indexes were calculated were considered achievable therapeutically. [2] In the checkerboard assays, a drop of up to 10-12 dilutions in the MIC of dicloxacillin sodium was observed when combined with amikacin compared to its MIC alone. [2] |
| ln Vivo |
When used in a murine peritonitis-sepsis model, dicloxacillin shows therapeutic activity, and all of the mice survive1–4.
In a mouse peritonitis model, a single subcutaneous dose of dicloxacillin resulted in a 1-log10 reduction in both intra- and extracellular bacterial counts after 4 h. Multiple dosing over 24 h increased efficacy to 2.5-log10 reduction extracellularly and 2-log10 reduction intracellularly. The fT/MIC index was the most predictive PK/PD parameter for both intra- and extracellular efficacy. [3] |
| Cell Assay |
Cell Line: Strains ATCC 25923 and E19977.
Concentration: 0-500 mg/L. Incubation Time: Up to 24 h. Result: EC50 values in ATCC 25923 and E19977 were found to be 0.06 and 0.50 mg/L, respectively. The antibacterial activity was determined using a broth microdilution method according to CLSI guidelines. The tested concentration range for dicloxacillin sodium was from 0.125 to 1024 mg/L. [2] Checkerboard synergy tests were performed in 96-well microtiter plates. Two-fold serial dilutions of dicloxacillin sodium and the companion antibiotic (amikacin) were dispensed in a checkerboard pattern. Each well contained 0.1 mL of the antimicrobial combination. Bacterial suspensions were adjusted to a 0.5 McFarland standard and diluted to yield a final inoculum of 3×10^5 to 5×10^5 CFU/mL. Plates were incubated overnight at 35°C. The MIC was defined as the lowest concentration that inhibited visible growth. Growth and sterility controls were included. Each isolate was tested twice. [2] |
| Animal Protocol |
Animal Model: Female outbred Swiss Webster mice (Murine peritonitis-sepsis model)[4].
Dosage: 125 mg/kg. Administration: IV injection, single doses. Result: All the mice survived. A mouse peritonitis model was used with female NMRI mice infected intraperitoneally with S. aureus (10^7.4 CFU in 0.5 mL). Dicloxacillin was administered subcutaneously 2 h post-infection in single or multiple doses. Peritoneal lavage was performed to collect intra- and extracellular bacteria for CFU quantification. Intra- and extracellular bacteria were separated using lysostaphin treatment and differential centrifugation. [3] |
| ADME/Pharmacokinetics |
Dicloxacillin exhibits nonlinear pharmacokinetic characteristics in NMRI mice, with a short half-life (19-30 minutes). Peak plasma concentrations are reached 9-24 minutes after subcutaneous administration. Protein binding is concentration-dependent and saturable, ranging from 70% to 93.9% in infected mice. Free drug concentrations are modeled using the square root of the total concentration. [3]
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| Toxicity/Toxicokinetics |
No cytotoxicity was observed in THP-1 macrophages after treatment with dicloxacillin at concentrations up to 500 mg/L for 24 hours (trypan blue exclusion method). At high drug concentrations, protein binding rates in infected mice were higher than in healthy mice. [3]
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| References |
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| Additional Infomation |
Dicloxacillin sodium monohydrate is a hydrate containing dicloxacillin sodium. Dicloxacillin sodium is the sodium salt form of dicloxacillin, a broad-spectrum semi-synthetic β-lactam antibiotic with bactericidal and anti-β-lactamase activity. Dicloxacillin sodium binds to penicillin-binding protein (PBP) located on the inner membrane of bacterial cell walls and inhibits the cross-linking of peptidoglycan (a key component of bacterial cell walls). This leads to the inhibition of bacterial cell wall synthesis, ultimately resulting in cell lysis. It is one of the few penicillin antibiotics resistant to penicillinase. Dicloxacillin sodium is a β-lactam antibiotic belonging to the penicillin class. [2] In this study, dicloxacillin sodium was used in combination with amikacin as a potential treatment for multidrug-resistant Staphylococcus aureus isolates from hospital infections. [2]
The study concluded that dicloxacillin sodium combined with amikacin is one of the best synergistic combinations for testing drug-resistant strains, but it also pointed out that in vitro synergistic results alone cannot predict clinical efficacy. [2] |
| Molecular Formula |
C19H17N3O5SCL2.NA+
|
|---|---|
| Molecular Weight |
493.31618
|
| Exact Mass |
509.019
|
| Elemental Analysis |
C, 44.72; H, 3.56; Cl, 13.89; N, 8.23; Na, 4.50; O, 18.81; S, 6.28
|
| CAS # |
13412-64-1
|
| Related CAS # |
Dicloxacillin sodium;343-55-5;Dicloxacillin;3116-76-5
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| PubChem CID |
23675786
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| Appearance |
Solid powder
|
| Boiling Point |
692.4ºC at 760mmHg
|
| Melting Point |
222-225°C
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| Flash Point |
372.5ºC
|
| LogP |
2.131
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
32
|
| Complexity |
752
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
[O-]C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2NC(C3=C(C)ON=C3C4=C(Cl)C=CC=C4Cl)=O)N1C2=O)=O.[Na+].O
|
| InChi Key |
SIGZQNJITOWQEF-VICXVTCVSA-M
|
| InChi Code |
InChI=1S/C19H17Cl2N3O5S.Na.H2O/c1-7-10(12(23-29-7)11-8(20)5-4-6-9(11)21)15(25)22-13-16(26)24-14(18(27)28)19(2,3)30-17(13)24;;/h4-6,13-14,17H,1-3H3,(H,22,25)(H,27,28);;1H2/q;+1;/p-1/t13-,14+,17-;;/m1../s1
|
| Chemical Name |
sodium (2S,5R,6R)-6-(3-(2,6-dichlorophenyl)-5-methylisoxazole-4-carboxamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate hydrate
|
| Synonyms |
Dicloxacillin sodium hydrate; BLP-1011; BRL-1702; P 1011; P-1011; P1011; MDI-PC
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| HS Tariff Code |
2934.99.03.00
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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, avoid exposure to moisture. |
| 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) |
DMSO : ~100 mg/mL ( ~195.95 mM )
Water : 25~100 mg/mL(~48.99 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (48.99 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 | 2.0271 mL | 10.1354 mL | 20.2708 mL | |
| 5 mM | 0.4054 mL | 2.0271 mL | 4.0542 mL | |
| 10 mM | 0.2027 mL | 1.0135 mL | 2.0271 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05073627 | COMPLETED | Drug: Dicloxacillin | Drug-drug Interaction Healthy Volunteers |
University of Southern Denmark | 2022-02-07 | Phase 1 |
| NCT05578482 | RECRUITING | Drug: Dicloxacillin Oral Capsule Drug: Elocon 0.1 % Topical Cream |
Atopic Dermatitis Atopic Dermatitis Eczema Atopic Dermatitis Flare |
Jacob Pontoppidan Thyssen | 2022-10-24 | Phase 4 |
| NCT02983890 | COMPLETED | Drug: Dicloxacillin Drug: Placebos |
Healthy | Per Damkier | 2016-10-06 | Phase 1 |
| NCT00037050 | COMPLETED | Drug: Linezolid Drug: Vancomycin Drug: Oxacillin Drug: Dicloxacillin |
Bacteremia Bacterial Infections Gram-Positive Bacterial Infections |
Pfizer | 2002-04 | Phase 3 |
| NCT04563325 | ACTIVE, NOT RECRUITING | Drug: Oral co-amoxiclav or oral dicloxacillin only Drug: IV ceftriaxon followed by oral co-amoxiclav or oral dicloxacillin |
Bone Infection Bone and Joint Infection Joint Infection Osteomyelitis Septic Arthritis |
Rigshospitalet, Denmark | 2020-09-15 | Phase 4 |
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