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| Targets |
Tetracycline
Cloxacillin sodium hydrate targets penicillin-binding proteins (PBPs) in the bacterial cell wall. It binds to and inactivates these enzymes, which are essential for bacterial cell wall synthesis. As a β-lactamase inhibitor, it resists degradation by beta-lactamase enzymes produced by certain bacteria, such as Staphylococcus aureus. |
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| ln Vitro |
For S. aureus 8325-4 and DU1090, cloxacillin sodium monohydrate (0–2048 µg/mL; 20–24 h) exhibits good antibacterial activity with MIC values of 0.125 µg/mL[1].
The hemolytic activity of Hlα is inhibited in vitro by cloxacillin sodium monohydrate (0.015625 μg/mL; 6 h). This inhibition is enhanced when combined with TZ and TZ. Additionally, cloxacillin sodium monohydrate suppresses the inflammatory response by preventing the activation of MAPKs, NF-кB, and NLRP3-related proteins[1]. In vitro, Cloxacillin sodium hydrate exhibits good antibacterial activity against S. aureus 8325-4 and DU1090 with MIC values of 0.125 µg/mL. It inhibits the hemolytic activity of Hlα at 0.015625 μg/mL. It suppresses the inflammatory response by preventing the activation of MAPKs, NF-кB, and NLRP3-related proteins. |
| ln Vivo |
Cloxacillin (HSDB-3042) (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]. 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. |
| Enzyme Assay |
Cloxacillin sodium hydrate is evaluated in cell-free assays for its ability to inhibit β-lactamase. The compound is incubated with β-lactamase and a substrate, and the inhibition of enzyme activity is measured. IC50 values are determined to quantify the potency of β-lactamase inhibition.
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| Cell Assay |
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 DU1090 and S. aureus 8325-4 with MIC values of 0.125 µg/mL. Cloxacillin sodium hydrate is assessed in cell-based assays using bacterial cultures. The compound is tested against various bacterial strains, and minimum inhibitory concentrations are determined. Its effects on bacterial growth and viability are evaluated. |
| Animal Protocol |
Animal Model: Eight weeks old; systemic S. aureus-induced arthritis model; female wildtype C57BL/6 mice)
Dosage: 7.5 mg/per (combines with 25 µg/per anti-IL-15 antibodies) Administration: intraperitoneal injection; started on day 3 (following bacterial inoculation) and continued every day until day 6. Result: demonstrated effects on bone erosions and severe synovitis when paired with anti-IL-15 antibodies. Cloxacillin sodium hydrate is administered orally or by injection in animal models to evaluate its antibacterial efficacy. In a peritonitis model, it protects mice from S. aureus infection. In an arthritis model, it reduces synovitis and bone erosions. Efficacy is assessed by measuring bacterial load, inflammatory markers, and tissue damage. |
| ADME/Pharmacokinetics |
Cloxacillin sodium hydrate has a molecular weight of 475.88 and a molecular formula of C19H17ClN3O5S·Na·H2O. It has a CAS number of 7081-44-9. The compound is a white, crystalline powder, soluble in 2.5 parts of water and in 30 parts of ethanol. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
Cloxacillin sodium hydrate is a semisynthetic penicillin and is generally well-tolerated. No detailed toxicity data is available beyond its known use as an antibiotic. It can cause contact dermatitis in sensitive individuals. It is a therapeutic agent and is available by prescription only.
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| References |
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| Additional Infomation |
Cloxacillin sodium is an organocalocyanate containing the cloxacillin(1-) ion. Cloxacillin sodium is the sodium salt of cloxacillin, a semi-synthetic, β-lactamase-resistant penicillin antibiotic with antibacterial activity. Cloxacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of bacterial cell walls, thereby preventing the cross-linking of peptidoglycan, a key component of the bacterial cell wall. This leads to the disruption of the bacterial cell wall, ultimately resulting in bacterial cell lysis. Anhydrous cloxacillin sodium is the anhydrous form of cloxacillin sodium salt. Cloxacillin is a semi-synthetic, β-lactamase-resistant penicillin antibiotic with antibacterial activity. Cloxacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of bacterial cell walls, thereby preventing the cross-linking of peptidoglycan (a key component of the bacterial cell wall). This leads to the disruption of the bacterial cell wall, ultimately resulting in bacterial cell lysis. Cloxacillin is a semi-synthetic antibiotic and a chlorinated derivative of oxacillin. See also: Cloxacillin (containing the active portion).
Cloxacillin sodium hydrate is also known as sodium cloxacillin monohydrate and oxacillin impurity E. It is a chlorinated derivative of oxacillin that shows β-lactamase-resistant antibiotic activity. It is effective against gram-positive organisms, particularly Staphylococcus aureus. It is a therapeutic agent. |
| Molecular Formula |
C19H17CLN3NAO5S
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| Molecular Weight |
457.8632
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| Exact Mass |
457.047
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| Elemental Analysis |
C, 49.84; H, 3.74; Cl, 7.74; N, 9.18; Na, 5.02; O, 17.47; S, 7.00
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| CAS # |
7081-44-9
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| Related CAS # |
Cloxacillin sodium;642-78-4;Cloxacillin;61-72-3
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| PubChem CID |
23675320
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| Appearance |
White to light yellow solid powder.
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| Boiling Point |
689.7ºC at 760 mmHg
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| Flash Point |
370.9ºC
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| LogP |
0.992
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
728
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| Defined Atom Stereocenter Count |
3
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| SMILES |
ClC1=C([H])C([H])=C([H])C([H])=C1C1C(=C(C([H])([H])[H])ON=1)C(N([H])[C@]1([H])C(N2[C@@]([H])(C(=O)[O-])C(C([H])([H])[H])(C([H])([H])[H])S[C@@]21[H])=O)=O.[Na+]
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| InChi Key |
InChI=1S/C19H18ClN3O5S.Na/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);/q;+1/p-1/t13-,14+,17-;/m1./s1
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| InChi Code |
InChI=1S/C19H18ClN3O5S.Na/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);/q;+1/p-1/t13-,14+,17-;/m1./s1
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| Chemical Name |
sodium (2S,5R,6R)-6-(3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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| Synonyms |
Cloxacilina; Cloxacilline; Cloxacillinum; Syntarpen; Tegopen, Cloxacillin sodium.
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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 : 55~100 mg/mL (115.57~210.14 mM )
Ethanol : ~25 mg/mL H2O : ~50 mg/mL (~105.07 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (5.25 mM) Solubility in Formulation 5: 100 mg/mL (210.14 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1841 mL | 10.9204 mL | 21.8407 mL | |
| 5 mM | 0.4368 mL | 2.1841 mL | 4.3681 mL | |
| 10 mM | 0.2184 mL | 1.0920 mL | 2.1841 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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