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Cloxacillin (HSDB-3042), a chlorinated derivative of Oxacillin, is a potent and orally bioactive antibacterial agent acting as a β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related protein.
| ln Vitro |
For S, cloxacillin (0–2048 µg/mL; 20–24 h) exhibits satisfactory antibacterial action. MIC values for aureus 8325-4 and DU1090 are both 0.125 µg/mL[1]. In vitro, cloxacillin (0.015625 μg/mL; 6 h) suppresses the hemolytic activity of Hlα, and this suppression is enhanced when combined with TZ and TZ. Additionally, cloxacillin inhibits the inflammatory response by preventing the activation of MAPKs, NF-кB, and proteins linked to NLRP3[1].
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| ln Vivo |
Mice are protected against S by cloxacillin (1.6125 mg/kg; sc; 12-h intervals for 72 h). When combined with thioridazine and tetracycline, aureus can cause peritonitis in vivo[1]. When combined with anti-IL-15 antibodies, cloxacillin (7.5 mg/per; ip; twice daily starting on day 3) results in less severe synovitis and less bone erosion[3].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: S. aureus 8325-4, S. aureus DU1090 (an Hlα-deleted strain) Tested Concentrations: 0-2048 µg/mL Incubation Duration: 20-24 h Experimental Results: Inhibited S. aureus 8325-4 and DU1090 with MIC values both of 0.125 μg/mL. Western Blot Analysis[1] Cell Types: S. aureus 8325-4 Tested Concentrations: 0.015625 μg/mL (combines with Thioridazine (TZ, 0.25 μg/mL) and Tetracycline (TC, 0.03125 μg/mL)). Incubation Duration: 6 h Experimental Results: Inhibited the expression of Hlα and the inhibition was more pronounced when combined with TZ and TC. Western Blot Analysis[1] Cell Types: RAW264.7 cells (exposes to S. aureus 8325-4/DU1090 or pure Hlα) Tested Concentrations: 0.015625 μg/mL (combines with TZ (0.25 μg/mL) and TC (0.03125 μg/mL)). Incubation Duration: 6 h Experimental Results: Inhibited the activation of MAPKs, NF -кB and NLRP3-related proteins thereby inhibiting the inflammatory response when combined with TC and TZ. |
| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse (6weeks old; peritonitis model)[1].
Doses: 1.6125 mg/kg (combines with TC (3.125 mg/kg) and TZ (25 mg/kg)) Route of Administration: subcutaneous (sc) injection; 12-h intervals for 72 h. Experimental Results: decreased the degree of inflammatory cell infiltration in the mouse lung tissue and alveolar structures tended to be normal. Dramatically decreased the pathological changes in spleen and liver tissue, as well as diminished the CFU counts of S. aureus in the peritoneal cavity. Animal/Disease Models: Female wildtype C57BL/6 mice (8weeks old; systemic S. aureus-induced arthritis model) Doses: 7.5 mg/per (combines with 25 µg/per anti-IL-15 antibodies) Route of Administration: intraperitoneal (ip)injection; twice (two times) daily from day 3 (after bacterial inoculation) and stopped at day 6. Experimental Results: demonstrated activities of reducing severe synovitis and bone erosions when combined with anti-IL-15 antibodies. |
| References |
[1]. Zhou H, et al. The combination of cloxacillin, thioridazine and tetracycline protects mice against Staphylococcus aureus peritonitis by inhibiting α-Hemolysin-induced MAPK/NF-κB/NLRP3 activation. Int J Biol Macromol. 2022 Feb 15;198:1-10.
[2]. Bergmann B, et al. Antibiotics with Interleukin-15 Inhibition Reduce Joint Inflammation and Bone Erosions but Not Cartilage Destruction in Staphylococcus aureus-Induced Arthritis. Infect Immun. 2018 Apr 23;86(5):e00960-17. [3]. Lupiola-Gómez PA, et al. Group 1 beta-lactamases of Aeromonas caviae and their resistance to beta-lactam antibiotics. Can J Microbiol. 2003 Mar;49(3):207-15. |
| Molecular Formula |
C19H18CLN3O5S
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|---|---|
| Molecular Weight |
435.88
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| CAS # |
61-72-3
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| Related CAS # |
Cloxacillin sodium monohydrate;7081-44-9;Cloxacillin sodium;642-78-4
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2NC(C3=C(C)ON=C3C4=CC=CC=C4Cl)=O)N1C2=O)O
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| InChi Key |
LQOLIRLGBULYKD-JKIFEVAISA-N
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| InChi Code |
InChI=1S/C19H18ClN3O5S/c1-8-11(12(22-28-8)9-6-4-5-7-10(9)20)15(24)21-13-16(25)23-14(18(26)27)19(2,3)29-17(13)23/h4-7,13-14,17H,1-3H3,(H,21,24)(H,26,27)/t13-,14+,17-/m1/s1
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| Chemical Name |
4-Thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(((3-(2-chlorophenyl)-5-methyl-4-isoxazolyl)carbonyl)amino)-3,3-dimethyl-7-oxo-, (2S-(2alpha,5alpha,6beta))-
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| Synonyms |
HSDB-3042Cloxacillin HSDB3042 HSDB 3042
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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 | 2.2942 mL | 11.4710 mL | 22.9421 mL | |
| 5 mM | 0.4588 mL | 2.2942 mL | 4.5884 mL | |
| 10 mM | 0.2294 mL | 1.1471 mL | 2.2942 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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