Cloxacillin sodium hydrate

Alias: Cloxacilina; Cloxacilline; Cloxacillinum; Syntarpen; Tegopen, Cloxacillin sodium.

Cat No.:V18556 Purity: ≥98%

COA Product Data Instructions for use SDS

Cloxacillin sodium hydrate Chemical Structure CAS No.: 7081-44-9
Product category: Bacterial

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Cloxacillin sodium hydrate:

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

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Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

Cloxacillin Sodium hydrate (HSDB-3042), 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.

Biological Activity I Assay Protocols (From Reference)

Targets

Tetracycline

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].

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.

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.

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.

References

[1]. 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]. 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]. Group 1 beta-lactamases of Aeromonas caviae and their resistance to beta-lactam antibiotics. Can J Microbiol. 2003 Mar;49(3):207-15.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C19H17CLN3NAO5S
Molecular Weight	457.8632
Elemental Analysis	C, 49.84; H, 3.74; Cl, 7.74; N, 9.18; Na, 5.02; O, 17.47; S, 7.00
CAS #	7081-44-9
Related CAS #	Cloxacillin sodium;642-78-4;Cloxacillin;61-72-3
Appearance	White to light yellow solid powder.
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+]
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
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
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
Synonyms	Cloxacilina; Cloxacilline; Cloxacillinum; Syntarpen; Tegopen, Cloxacillin sodium.
HS Tariff Code	2934.99.9001
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)

Solubility Data

Solubility (In Vitro)	DMSO : 55~100 mg/mL (115.57~210.14 mM ) Ethanol : ~25 mg/mL H2O : ~50 mg/mL (~105.07 mM)
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. 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 corn oil and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO : 55~100 mg/mL (115.57~210.14 mM )
Ethanol : ~25 mg/mL
H2O : ~50 mg/mL (~105.07 mM)

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.
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 corn oil and mix evenly.

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.

(Please use freshly prepared in vivo formulations for optimal results.)

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.

Calculator

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

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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.

Note： (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.

Biological Data

The addition of anti-IL-15 antibodies (aIL-15ab) to antibiotics does not adversely affect the clinical course of S. [2]. 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.

Antibiotics and IL-15 inhibition reduce synovitis, bone erosions, and osteoclast numbers in the joint but do not influence cartilage destruction during S. aureus-induced arthritis. [2]. 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.

The combination therapy of aIL-15ab and antibiotics increases the proportion of inflammatory monocytes in the draining lymph nodes of the knee joints during S. aureus-induced arthritis. [2]. 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.