[CAS NO. 7081-44-9] Cloxacillinsodiummonohydrate
PRODUCTS SPECIFICATIONS [7081-44-9]
DESCRIPTION [7081-44-9]
Overview
| MDL | MFCD00150735 |
|---|---|
| Molecular Weight | 475.88 |
| Molecular Formula | C19H19ClN3NaO6S |
| SMILES | O=C(C(C(C(C=CC=C1)=C1Cl)=NO2)=C2C)N[C@H]3[C@](SC(C)(C)[C@@H]4C(O[Na])=O)([H])N4C3=O.O |
3 Publications Citing Use of MCE
Summary
IC50 & Target
|
Tetracycline |
In Vitro
Cloxacillin sodium monohydrate (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 sodium monohydrate (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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | S. aureus 8325-4, S. aureus DU1090 (an Hlα-deleted strain) |
| Concentration: | 0-2048 µg/mL |
| Incubation Time: | 20-24 h |
| Result: | Inhibited S. aureus 8325-4 and DU1090 with MIC values both of 0.125 µg/mL. |
Western Blot Analysis [1]
| Cell Line: | S. aureus 8325-4 |
| Concentration: | 0.015625 μg/mL (combines with Thioridazine (TZ, 0.25 μg/mL) and Tetracycline (TC, 0.03125 μg/mL)). |
| Incubation Time: | 6 h |
| Result: | Inhibited the expression of Hlα and the inhibition was more pronounced when combined with TZ and TC. |
Western Blot Analysis [1]
| Cell Line: | RAW264.7 cells (exposes to S. aureus 8325-4/DU1090 or pure Hlα) |
| Concentration: | 0.015625 μg/mL (combines with TZ (0.25 μg/mL) and TC (0.03125 μg/mL)). |
| Incubation Time: | 6 h |
| 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 sodium monohydrate (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 sodium monohydrate (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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female BALB/c mice (6-week-old; peritonitis model) [1] . |
| Dosage: | 1.6125 mg/kg (combines with TC (3.125 mg/kg) and TZ (25 mg/kg)) |
| Administration: | Subcutaneous injection; 12-h intervals for 72 h. |
| 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. |
| Animal Model: | Female wildtype C57BL/6 mice (8-week-old; systemic S. aureus -induced arthritis model) |
| Dosage: | 7.5 mg/per (combines with 25 µg/per anti-IL-15 antibodies) |
| Administration: | Intraperitoneal injection; twice daily from day 3 (after bacterial inoculation) and stopped at day 6. |
| Result: | Showed activities of reducing severe synovitis and bone erosions when combined with anti-IL-15 antibodies. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01792804 | Heinrich-Heine University, Duesseldorf|German Research Foundation |
Staphylococcus Aureus Infection
|
December 2013 | Phase 3 |
| NCT00129688 | Khon Kaen University|National Research Council of Thailand |
Neutropenia|Cancer|Fever
|
April 2002 | Not Applicable |
| NCT01875263 | Fundación Pública Andaluza Progreso y Salud|Andalusian Network for Design and Translation of Advanced Therapies |
Staphylococcus
|
May 2013 | Phase 3 |
| NCT03248063 | Assistance Publique - Hôpitaux de Paris |
Bacteremia Due to Methicillin Susceptible Staphylococcus Aureus
|
September 5, 2018 | Not Applicable |
| NCT00062647 | Cumberland Pharmaceuticals |
Gram-Positive Bacterial Infections
|
August 2003 | Phase 2 |
| NCT03246360 | Centre Hospitalier Universitaire de Nice |
Infection|Methicillin Susceptible Staphylococcus Aureus Infection|Cloxacillin Treatment
|
November 23, 2017 | Not Applicable |
| NCT00885300 | Shiraz University of Medical Sciences |
Double Lumen Infection|Hemodialysis
|
January 2008 | Not Applicable |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL ( 210.14 mM ; Need ultrasonic)
H 2 O : 50 mg/mL ( 105.07 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1014 mL | 10.5069 mL | 21.0137 mL |
| 5 mM | 0.4203 mL | 2.1014 mL | 4.2027 mL |
| 10 mM | 0.2101 mL | 1.0507 mL | 2.1014 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (210.14 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution
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.
Synonyms