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).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 92.38%
- CAS 番号: 102961-72-8
- 分子式: C83H88Cl2N8O29
- 分子量:1732.53
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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Glycopeptide |
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.
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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 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%).
化学情報
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CAS 番号 102961-72-8
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性状 Solid
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分子量 1732.53
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
純度とドキュメンテーション
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データシート (293 KB)
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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-107833 関連分類
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