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Description: Cloxacillin Sodium (HSDB-3042 Sodium), a semi-synthetic and 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 |
S responds well to cloxacillin sodium (0–2048 µg/mL; 20–24 h) in terms of antibacterial activity. MIC values for aureus 8325-4 and DU1090 are both 0.125 µg/mL[1]. When coupled with TZ and TZ, cloxacillin sodium (0.015625 μg/mL; 6 h) not only more strongly inhibits the hemolytic activity of Hlα in vitro but also suppresses the inflammatory response by preventing the activation of MAPKs, NF-кB, and NLRP3-related proteins[1].
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| ln Vivo |
Mice are protected against S by cloxacillin sodium (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 sodium (7.5 mg/per; ip; twice daily from day 3 for 3 days) causes less severe synovitis and decreases bone erosions[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 (8-week- 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 |
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| Additional Infomation |
Cloxacillin sodium is an organic sodium salt. It contains a cloxacillin(1-).
Cloxacillin Sodium is the sodium salt of cloxaclliin, a semisynthetic beta-lactamase resistant penicillin antibiotic with antibacterial activity. Cloxacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall, thereby preventing the cross-linkage of peptidoglycans, which are critical components of the bacterial cell wall. This leads to an interruption of the bacterial cell wall and causes bacterial cell lysis. Cloxacillin Sodium Anhydrous is the anhydrous form of the sodium salt of cloxacillin, a semisynthetic beta-lactamase resistant penicillin antibiotic with antibacterial activity. Cloxacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall, thereby preventing the cross-linkage of peptidoglycans, which are critical components of the bacterial cell wall. This leads to an interruption of the bacterial cell wall and causes bacterial cell lysis. A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN. See also: Cloxacillin (has active moiety). |
| Molecular Formula |
C19H17CLN3NAO5S
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| Molecular Weight |
457.86
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| Exact Mass |
475.058
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| CAS # |
642-78-4
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| Related CAS # |
Cloxacillin sodium monohydrate;7081-44-9;Cloxacillin;61-72-3
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| PubChem CID |
23675320
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| Appearance |
White to off-white solid powder
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| Melting Point |
170ºC
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| LogP |
1.542
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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 |
CC1=C(C(=NO1)C2=CC=CC=C2Cl)C(=O)N[C@H]3[C@@H]4N(C3=O)[C@H](C(S4)(C)C)C(=O)[O-].[Na+]
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| InChi Key |
SCLZRKVZRBKZCR-SLINCCQESA-M
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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-methyl-1,2-oxazole-4-carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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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: 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 (~218.41 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.46 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 (5.46 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 (5.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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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