Cefuroxime axetil

Name: Cefuroxime axetil
Brand: MedChemExpress
SKU: HY-B1325
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1325 Purity: 99.53%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

Cefuroxime axetil is an orally effective broad-spectrum β-lactam antibiotic that targets bacterial penicillin-binding proteins (PBPs, such as PBP3 and PBP1). Cefuroxime axetil inhibits cell wall synthesis, leading to bacterial lysis and death, with a minimum inhibitory concentration (MIC) of 0.12-4 mg/L for non-typeable Haemophilus influenzae (NTHi). Cefuroxime axetil is hydrolyzed by esterase to the active ingredient Cefuroxime (HY-B1256A) after oral absorption. Topical administration of Cefuroxime via bioadhesive nanoparticles (BNPs) can prolong the drug's retention time in the middle ear (≥7 days). Cefuroxime axetil can be used in the study of otitis media (especially NTHi infection). Cefuroxime axetil can achieve precise antibacterial effects through oral or topical nano-delivery systems, reducing systemic exposure and the risk of antibiotic resistance.

For research use only. We do not sell to patients.

Cefuroxime axetil Chemical Structure

CAS No. : 64544-07-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Cefuroxime axetil:

Cefuroxime sodium In-stock
Cefuroxime axetil (Standard) Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

β-lactam

In Vitro

Kinase activity assay:
Cefuroxime axetil has a potent inhibitory effect on penicillin-binding proteins (PBPs) of Gram-positive bacteria (such as Streptococcus pneumoniae and Streptococcus pyogenes) and Gram-negative bacteria (such as Haemophilus influenzae and Moraxella catarrhalis). The MIC₉₀ for penicillin-sensitive Streptococcus pneumoniae is ≤0.25 mg/L, and the MIC₉₀ for β-lactamase-producing Haemophilus influenzae and Moraxella catarrhalis are 1-2 mg/L and 0.5 mg/L, respectively[1].
In vitro antibacterial tests:
Cefuroxime axetil has limited activity against penicillin-resistant Streptococcus pneumoniae (MIC₉₀=2-8 mg/L) and methicillin-susceptible Staphylococcus aureus (MIC₉₀=2-4 mg/L), with highly sensitive to Neisseria gonorrhoeae (MIC₉₀=0.06-0.125 mg/L)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Acute otitis media mouse model:
Cefuroxime axetil (30 mg/kg; oral gavage; twice daily; 5-10 days) significantly inhibits the bacterial load in the middle ear in the acute otitis media model induced by non-typical Haemophilus influenzae (NTHi) in C57BL/6J female mice (6-8 weeks old). The middle ear effusion disappeares after 7 days, and histopathology shows a significant reduction in inflammation. The blood concentration is below the detection limit without systemic toxicity^[1].
Community-acquired pneumonia (CAP) rat model:
Cefuroxime axetil (20 mg/kg/day; oral; twice daily; 7-14 days) shows comparable bacterial clearance to the control group in the adult rat CAP model compared with sequential treatment with intravenous cefuroxime (HY-B1256A) with good gastrointestinal tolerance^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female C57BL/6J mice (6-8 weeks old) with NTHi-induced acute otitis media model^[1]
Dosage:	30 mg/kg
Administration:	Oral gavage, twice daily, for 5-10 days
Result:	Reduced bacterial colony-forming units (CFU) in middle ear effusion by >99% compared to vehicle control. At day 7, clinical signs of inflammation (e.g., tympanic membrane redness, effusion) resolved in 93% of treated mice, with no histopathological evidence of tissue damage. Remained serum drug concentrations undetectable, confirming minimal systemic exposure.

Animal Model:	Adult Sprague-Dawley rats (~200-250 g) with community-acquired pneumonia model^[1]
Dosage:	250 mg or 500 mg (tablet formulation)
Administration:	Oral administration, twice daily, for 7-14 days
Result:	Resulted clinical cure rates of 85% (250 mg group) and 94% (500 mg group) at end-of-treatment, comparable to intravenous cefuroxime followed by oral cefuroxime axetil (sequential therapy). Bacterial eradication rates were 89%-95% for Streptococcus pneumoniae and Haemophilus influenzae isolates, without significant differences in safety profiles compared to comparators. Gastrointestinal adverse events (e.g., diarrhea) occurred in <5% of treated animals.

Clinical Trial

Molecular Weight

510.47

Formula

C₂₀H₂₂N₄O₁₀S

CAS No.

64544-07-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(C(N12)=C(COC(N)=O)CS[C@]2([H])[C@H](NC(/C(C3=CC=CO3)=N\OC)=O)C1=O)OC(OC(C)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (244.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9590 mL	9.7949 mL	19.5898 mL
5 mM	0.3918 mL	1.9590 mL	3.9180 mL
10 mM	0.1959 mL	0.9795 mL	1.9590 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.53%

Select Batch:

Data Sheet (283 KB) SDS (557 KB)

COA (255 KB) HNMR (297 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Scott LJ, et al. Cefuroxime axetil: an updated review of its use in the management of bacterial infections. Drugs. 2001;61(10):1455-500. [Content Brief]

[2]. Lin H, et al. In Vivo Evaluation of Cefuroxime Axetil-Loaded Bioadhesive Nanoparticles to Treat Haemophilus influenzae-Induced Otitis Media. Front Bioeng Biotechnol. 2022 Apr 29;10:884797. [Content Brief]

[3]. Dafale Nishant A, et al. Development and validation of microbial bioassay for the quantification of potency of the antibiotic cefuroxime axetil. Analytical Methods 5.3 (2013): 690-698.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9590 mL	9.7949 mL	19.5898 mL	48.9745 mL
	5 mM	0.3918 mL	1.9590 mL	3.9180 mL	9.7949 mL
	10 mM	0.1959 mL	0.9795 mL	1.9590 mL	4.8974 mL
	15 mM	0.1306 mL	0.6530 mL	1.3060 mL	3.2650 mL
	20 mM	0.0979 mL	0.4897 mL	0.9795 mL	2.4487 mL
	25 mM	0.0784 mL	0.3918 mL	0.7836 mL	1.9590 mL
	30 mM	0.0653 mL	0.3265 mL	0.6530 mL	1.6325 mL
	40 mM	0.0490 mL	0.2449 mL	0.4897 mL	1.2244 mL
	50 mM	0.0392 mL	0.1959 mL	0.3918 mL	0.9795 mL
	60 mM	0.0326 mL	0.1632 mL	0.3265 mL	0.8162 mL
	80 mM	0.0245 mL	0.1224 mL	0.2449 mL	0.6122 mL
	100 mM	0.0196 mL	0.0979 mL	0.1959 mL	0.4897 mL