A40926
Based on 1 Customer Validation
A40926 is a glycopeptide antibiotic that targets the bacterial cell wall peptidoglycan precursor D-alanyl-D-alanine (D-Ala-D-Ala). A40926 irreversibly inhibits cell wall synthesis by competitively binding to this target, and has high bactericidal activity against Gram-positive bacteria (such as Staphylococcus, Streptococcus) and Neisseria gonorrhoeae, with MIC=0.06-2 μg/mL, and is also effective against penicillin-resistant strains. A40926 blocks peptidoglycan cross-linking, destroys cell wall integrity, and causes bacterial lysis and death. A40926 has a fat-soluble fatty acid structure, which can increase serum concentrations and prolong the duration of action (e.g., the terminal half-life in rats is 61.22 h).
For research use only. We do not sell to patients.
- Purity : 92.38%
- CAS No.: 102961-72-8
- Formula: C83H88Cl2N8O29
- Molecular Weight:1732.53
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
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Glycopeptide |
In Vitro
A40926 shows strong inhibitory activity against Gram-positive bacteria (such as Staphylococcus aureus and Streptococcus) and Neisseria gonorrhoeae, with MIC=0.004-32 μg/mL. The median MIC against clinical isolates of Neisseria gonorrhoeae is 1 μg/mL, which is significantly lower than Teicoplanin (HY-A0097) and Vancomycin (HY-B0671)[1].
A40926 (4-16 μg/mL; 5 h) could kill 99.9%-99.99% of clinical isolates within 5 h at concentrations 4 to 8 times the MIC, including penicillin-resistant and spectinomycin (HY-B1828)-resistant strains, showing rapid bactericidal activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Neisseria gonorrhoeae, Streptococcus pyogenes, Streptococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis
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Concentration:MIC
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Incubation Time:
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Result:Exhibited antibacterial activity with MIC values of 2 μg/mL (Neisseria gonorrhoeae), 0.06 μg/mL (Streptococcus pyogenes), 0.06 μg/mL (Streptococcus faecalis), 0.06 μg/mL (Staphylococcus aureus), 0.06 μg/mL (Staphylococcus epidermidis), respectively.
In Vivo
In the pharmacokinetic model of male CD rats, A40926 (10 mg/kg; iv/sc; single dose) shows decayed plasma concentration in a power function after intravenous injection, with a terminal half-life of 61.22 h, a subcutaneous bioavailability of nearly 90%, and a urinary excretion rate of 35.9% at 120 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice (male and female, 18-22 g) infected with Staphylococcus aureus, Streptococcus pyogenes, or Streptococcus pneumoniae[1]
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Dosage:10 mg/kg (dissolved in 10% DMSO, 40% PEG 300, 5% Tween-80, and 45% saline)
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Administration:Subcutaneous injection, single dose
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Result:Demonstrated protective efficacy against systemic infections caused by gram-positive pathogens, with ED50 values of 1.9 mg/kg for S. aureus, 0.33 mg/kg for S. pyogenes, and 0.38 mg/kg for S. pneumoniae.
Although slightly less effective than Teicoplanin (HY-A0097) in survival rates, achieved peak serum concentrations of 128 μg/mL and maintained effective levels (>1 μg/mL) for over 72 h, indicating prolonged exposure compared to Teicoplanin (HY-A0097).
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Animal Model:Male CD rats (161-185 g) for pharmacokinetic analysis[2]
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Dosage:10 mg/kg (formulated in 10% DMSO and 90% corn oil for s.c.)
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Administration:Intravenous or subcutaneous injection, single dose, 1 cycle.
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Result:Displayed a tri-exponential plasma concentration profile with a terminal half-life of 61.22 h, mean residence time of 84.5 h, and total clearance of 0.11 L/h/kg.
Subcutaneous injection resulted in rapid absorption (Tmax=2 h) and high bioavailability (~90%).
Urinary excretion accounted for 35.9% of the administered dose within 120 h, primarily as unchanged drug, while fecal excretion was minimal (<5%).
Chemical Information
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CAS No. 102961-72-8
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Appearance Solid
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Molecular Weight 1732.53
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Formula C83H88Cl2N8O29
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Color White to off-white
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SMILES
ClC1=CC(C(O)C(C(NC(C(O)=O)C(C=C(O)C=C2O[C@@H]3[C@@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O3)=C2C4=C(O)C=CC(C5NC(C6NC(C(C7=C(Cl)C(O)=CC(O8)=C7)NC(C9NC(C(C%10=CC8=C(O)C=C%10)NC)=O)=O)=O)=O)=C4)=O)NC5=O)=CC=C1OC%11=CC6=CC(OC%12=CC=C(C9)C=C%12)=C%11O[C@@H]%13O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]%13NC(CCCCCCCCC(C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 5.88 mg/mL (3.39 mM; ultrasonic and warming and heat to 20°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.59 mg/mL (0.34 mM); Clear solution
This protocol yields a clear solution of ≥ 0.59 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.9 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.59 mg/mL (0.34 mM); Clear solution
This protocol yields a clear solution of ≥ 0.59 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.9 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
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Bacterial live/dead nucleic-acid viability staining
The LIVE/DEAD bacterial viability staining method is based on differential permeability of nucleic-acid-binding fluorescent dyes, most commonly SYTO 9 and propidium iodide (PI), which enables discrimination of bacterial populations with intact versus compromised cytoplasmic membranes. SYTO 9 penetrates both intact and damaged bacterial membranes and binds nucleic acids to produce green fluorescence, whereas propidium iodide penetrates only cells with compromised membranes and fluoresces red while also reducing SYTO 9 signal through competitive binding and fluorescence interactions. The resulting fluorescence pattern is interpreted as a proxy for membrane integrity, which is widely used as an indicator of bacterial viability in microscopy, flow cytometry, and spectroscopic platforms. However, mechanistic studies show that SYTO 9 and PI interactions involve displacement and fluorescence resonance energy transfer effects, which can influence signal interpretation depending on dye ratios a
Purity & Documentation
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Data Sheet (293 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Goldstein BP, et al. A40926, a new glycopeptide antibiotic with anti-Neisseria activity.Antimicrob Agents Chemother. 1987 Dec;31(12):1961-6. [Content Brief]
[2]. Bernareggi A, et al. Pharmacokinetics of A40926 in rats after single intravenous and subcutaneous doses. Antimicrob Agents Chemother. 1988 Feb;32(2):246-9. [Content Brief]
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.5772 mL | 2.8860 mL | 5.7719 mL | 14.4298 mL |
A40926 Related Classifications
HY-107833 Related Classifications
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