Cloxacillin
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Cloxacillin is an orally active antibacterial agent and 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 proteins.
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- No. CAS: 61-72-3
- Fòrmula: C19H18ClN3O5S
- Peso molecular:435.88
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Publications Citing Use of MedChemExpress (MCE) Cloxacillin
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Actividad biológica
Descripciòn
Cloxacillin is an orally active antibacterial agent and 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 proteins[1][2][3].
IC50 & Target
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Tetracycline |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Calu-3 | EC50 |
0.39 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against intracellular hospital acquired methicillin-resistant Staphylococcus aureus ATCC 33591 infected in human Calu3 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
Antimicrobial activity against intracellular hospital acquired methicillin-resistant Staphylococcus aureus ATCC 33591 infected in human Calu3 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
|
[PMID: 18519727] |
| Calu-3 | EC50 |
0.52 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against intracellular beta-lactamase negative methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human Calu3 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
Antimicrobial activity against intracellular beta-lactamase negative methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human Calu3 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
|
[PMID: 18519727] |
| CHO | IC50 |
30.9 μM
Compound: Cloxacillin
|
Inhibition of mouse OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake over 20 mins
Inhibition of mouse OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake over 20 mins
|
[PMID: 23344796] |
| Sf21 | IC50 |
219.7 μM
Compound: Cloxacillin
|
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
[PMID: 21965623] |
| Sf21 | IC50 |
376.7 μM
Compound: Cloxacillin
|
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
[PMID: 21965623] |
| THP-1 | EC50 |
0.26 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus ATCC 33591 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus ATCC 33591 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
|
[PMID: 18519727] |
| THP-1 | EC50 |
0.27 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against beta-lactamase negative methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
Antimicrobial activity against beta-lactamase negative methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
|
[PMID: 18519727] |
| THP-1 | EC50 |
0.32 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against intracellular hospital acquired methicillin-resistant Staphylococcus aureus ATCC 33591 activated infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
Antimicrobial activity against intracellular hospital acquired methicillin-resistant Staphylococcus aureus ATCC 33591 activated infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
|
[PMID: 18519727] |
| THP-1 | EC50 |
0.43 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against intracellular beta-lactamase negative methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in activated human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
Antimicrobial activity against intracellular beta-lactamase negative methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in activated human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 7.4
|
[PMID: 18519727] |
| THP-1 | EC50 |
10.8 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against Panton-valentine leukocidin positive community acquired methicillin-resistant Staphylococcus aureus N4042228 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
Antimicrobial activity against Panton-valentine leukocidin positive community acquired methicillin-resistant Staphylococcus aureus N4042228 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
|
[PMID: 18519727] |
| THP-1 | EC50 |
2.74 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against constitutive beta-lactamase negative methicillin-resistant Staphylococcus aureus COL NRS100 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
Antimicrobial activity against constitutive beta-lactamase negative methicillin-resistant Staphylococcus aureus COL NRS100 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
|
[PMID: 18519727] |
| THP-1 | EC50 |
3.14 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against Panton-valentine leukocidin positive community acquired methicillin-resistant Staphylococcus aureus N4090440 obtained from wound infection of patient infected in human THP-1 cells assessed as decrease in bacterial growth aft
Antimicrobial activity against Panton-valentine leukocidin positive community acquired methicillin-resistant Staphylococcus aureus N4090440 obtained from wound infection of patient infected in human THP-1 cells assessed as decrease in bacterial growth aft
|
[PMID: 18519727] |
| THP-1 | EC50 |
3.63 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against hospital acquired methicillin-resistant and vancomycin-intermediate Staphylococcus aureus VRS2 obtained from wound, skin and soft tissue infection of patient infected in human THP-1 cells assessed as decrease in bacterial gr
Antimicrobial activity against hospital acquired methicillin-resistant and vancomycin-intermediate Staphylococcus aureus VRS2 obtained from wound, skin and soft tissue infection of patient infected in human THP-1 cells assessed as decrease in bacterial gr
|
[PMID: 18519727] |
| THP-1 | EC50 |
3.96 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against hospital acquired methicillin-resistant and vancomycin-intermediate Staphylococcus aureus NRS18 obtained from wound, skin and soft tissue infection of patient infected in human THP-1 cells assessed as decrease in bacterial g
Antimicrobial activity against hospital acquired methicillin-resistant and vancomycin-intermediate Staphylococcus aureus NRS18 obtained from wound, skin and soft tissue infection of patient infected in human THP-1 cells assessed as decrease in bacterial g
|
[PMID: 18519727] |
| THP-1 | EC50 |
4.25 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus ATCC 33591 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus ATCC 33591 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
|
[PMID: 18519727] |
| THP-1 | EC50 |
4.44 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against beta-lactamase negative methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
Antimicrobial activity against beta-lactamase negative methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
|
[PMID: 18519727] |
| THP-1 | EC50 |
5.33 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against hospital acquired methicillin-resistant and vancomycin-intermediate Staphylococcus aureus NRS126 obtained from bloodstream infection of patient infected in human THP-1 cells assessed as decrease in bacterial growth after 24
Antimicrobial activity against hospital acquired methicillin-resistant and vancomycin-intermediate Staphylococcus aureus NRS126 obtained from bloodstream infection of patient infected in human THP-1 cells assessed as decrease in bacterial growth after 24
|
[PMID: 18519727] |
| THP-1 | EC50 |
5.67 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus HMC546 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus HMC546 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
|
[PMID: 18519727] |
| THP-1 | EC50 |
6.07 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against Panton-valentine leukocidin positive community acquired methicillin-resistant Staphylococcus aureus NRS192 obtained from patient with pneumonia and septic arthritis infected in human THP-1 cells assessed as decrease in bacte
Antimicrobial activity against Panton-valentine leukocidin positive community acquired methicillin-resistant Staphylococcus aureus NRS192 obtained from patient with pneumonia and septic arthritis infected in human THP-1 cells assessed as decrease in bacte
|
[PMID: 18519727] |
| THP-1 | EC50 |
6.99 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against animal acquired methicillin-resistant Staphylococcus aureus N7112046 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
Antimicrobial activity against animal acquired methicillin-resistant Staphylococcus aureus N7112046 infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
|
[PMID: 18519727] |
| THP-1 | EC50 |
8.51 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus N4120210 obtained from urinary tract infection of patient infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus N4120210 obtained from urinary tract infection of patient infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
|
[PMID: 18519727] |
| THP-1 | EC50 |
9.26 mg/L
Compound: Cloxacillin
|
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus N4120032 obtained from wound infection opf patient infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus N4120032 obtained from wound infection opf patient infected in human THP-1 cells assessed as decrease in bacterial growth after 24 hrs at pH 5.5
|
[PMID: 18519727] |
In Vitro
Cloxacillin (0-2048 µg/mL; 20-24 h) shows good antibacterial activity for S. aureus 8325-4 and DU1090 with MIC values both of 0.125 µg/mL[1].
Cloxacillin (0.015625 μg/mL; 6 h) inhibits the hemolytic activity of Hlα in vitro, and this inhibition is not only more pronounced when combined with TZ and TZ, but also suppresses the inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
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Cell Line:S. aureus 8325-4, S. aureus DU1090 (an Hlα-deleted strain)
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Concentration:0-2048 µg/mL
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Incubation Time:20-24 h
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Result:Inhibited S. aureus 8325-4 and DU1090 with MIC values both of 0.125 µg/mL.
Western Blot Analysis[1]
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Cell Line:S. aureus 8325-4
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Concentration:0.015625 μg/mL (combines with Thioridazine (TZ, 0.25 μg/mL) and Tetracycline (TC, 0.03125 μg/mL)).
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Incubation Time:6 h
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Result:Inhibited the expression of Hlα and the inhibition was more pronounced when combined with TZ and TC.
Western Blot Analysis[1]
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Cell Line:RAW264.7 cells (exposes to S. aureus 8325-4/DU1090 or pure Hlα)
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Concentration:0.015625 μg/mL (combines with TZ (0.25 μg/mL) and TC (0.03125 μg/mL)).
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Incubation Time:6 h
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Result:Inhibited the activation of MAPKs, NF-кB and NLRP3-related proteins thereby inhibiting the inflammatory response when combined with TC and TZ.
In Vivo
Cloxacillin (1.6125 mg/kg; s.c.; 12-h intervals for 72 h) protects mice from S. aureus peritonitis in vivo when combines with Thioridazine and Tetracycline[1].
Cloxacillin (7.5 mg/per; i.p.; twice daily from day 3 for 3 days) develops less severe synovitis and reduces bone erosions when combines with anti-IL-15 antibodies[3].
Cloxacillin (7.5 mg/per; i.p.; twice daily from day 3 for 3 days) develops less severe synovitis and reduces bone erosions when combines with anti-IL-15 antibodies[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (6-week-old; peritonitis model)[1].
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Dosage:1.6125 mg/kg (combines with TC (3.125 mg/kg) and TZ (25 mg/kg))
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Administration:Subcutaneous injection; 12-h intervals for 72 h.
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Result:Reduced the degree of inflammatory cell infiltration in the mouse lung tissue and alveolar structures tended to be normal.
Significantly reduced the pathological changes in spleen and liver tissue, as well as decreased the CFU counts of S. aureus in the peritoneal cavity.
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Animal Model:Female wildtype C57BL/6 mice (8-week-old; systemic S. aureus-induced arthritis model)
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Dosage:7.5 mg/per (combines with 25 µg/per anti-IL-15 antibodies)
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Administration:Intraperitoneal injection; twice daily from day 3 (after bacterial inoculation) and stopped at day 6.
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Result:Showed activities of reducing severe synovitis and bone erosions when combined with anti-IL-15 antibodies.
Chemical Information
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No. CAS 61-72-3
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Peso molecular 435.88
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Fòrmula C19H18ClN3O5S
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SMILES
O=C(C1=C(C)ON=C1C2=C(C=CC=C2)Cl)N[C@H]3[C@]4([H])N([C@@H](C(O)=O)C(C)(C)S4)C3=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
The combination of cloxacillin, thioridazine and tetracycline protects mice against Staphylococcus aureus peritonitis by inhibiting α-Hemolysin-induced MAPK/NF-κB/NLRP3 activation. [Abstract]2022 Feb 15:198:1-10. PMID: 34963621 -
Biomed Res Int
In Vitro Activity of β-Lactams in Combination with β-Lactamase Inhibitors against Mycobacterium tuberculosis Clinical Isolates. [Abstract]2018 Jul 2:2018:3579832. PMID: 30065936 -
Chemosphere
Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]2019 Jun:225:378-387. PMID: 30884299
Pureza y Documentación
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Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
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Cloxacillin Related Classifications
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