Pilabactam sodium
Based on 1 Customer Validation
Pilabactam (ANT3310) sodium is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). Pilabactam sodium potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). Pilabactam sodium can be used in the research of bacterial infection.
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- Purity: 99.54%
- CAS No.: 2410688-61-6
- 화학식: C6H8FN2NaO5S
- 분자량:262.19
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | CC50 |
>100 μM
Compound: 21; ANT3310
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Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
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[PMID: 33306385] |
Pilabactam sodium (Compound 21, 0.006 to 3 000 nM, 10 min) inhibits a series of Serine β-Lactamase (AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2), with IC50 values ranging from 1 nM to 175 nM[1].
Pilabactam sodium shows a low in vitro cytotoxicity (IC50: > 100 μM) in HepG2 cell, cardiotoxicity (inhibition of the hERG potassium ion channel), and genotoxicity (Ames test)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pilabactam sodium (intravenous injection, 1 mg/kg, Male Swiss albino mice) shows a T1/2 value of 0.64 h, AUC value of 412 ng h/mL, and Cl value of 40 mL/min/kg (pharmacokinetic assay)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine thigh infection model[1]
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Dosage:25, 50, and 100 mg/kg
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Administration:Intravenous injection, at 1, 3, 5, and 7 h postinfection
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Result:Reduced bacterial burdens (colony forming units, CFU) in a dose-dependent manner to levels below that of the initial starting inoculum at the highest dose, when treated with the combination of MEM.
Chemical Information
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CAS No. 2410688-61-6
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Appearance Solid
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분자량 262.19
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화학식 C6H8FN2NaO5S
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Color White to light yellow
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SMILES
O=S(ON1[C@H]2C[N@]([C@@H](CC2)F)C1=O)(O[Na])=O
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Synonyms
ANT3310 sodium
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (190.70 mM; ultrasonic and warming and heat to 60°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)
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: ≥ 1.67 mg/mL (6.37 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (6.37 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
순도&문서
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. David T Davies, et al. Discovery of ANT3310, a Novel Broad-Spectrum Serine β-Lactamase Inhibitor of the Diazabicyclooctane Class, Which Strongly Potentiates Meropenem Activity against Carbapenem-Resistant Enterobacterales and Acinetobacter baumannii. J Med Chem. 2020 Dec 24;63(24):15802-15820. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8140 mL | 19.0701 mL | 38.1403 mL | 95.3507 mL |
| 5 mM | 0.7628 mL | 3.8140 mL | 7.6281 mL | 19.0701 mL | |
| 10 mM | 0.3814 mL | 1.9070 mL | 3.8140 mL | 9.5351 mL | |
| 15 mM | 0.2543 mL | 1.2713 mL | 2.5427 mL | 6.3567 mL | |
| 20 mM | 0.1907 mL | 0.9535 mL | 1.9070 mL | 4.7675 mL | |
| 25 mM | 0.1526 mL | 0.7628 mL | 1.5256 mL | 3.8140 mL | |
| 30 mM | 0.1271 mL | 0.6357 mL | 1.2713 mL | 3.1784 mL | |
| 40 mM | 0.0954 mL | 0.4768 mL | 0.9535 mL | 2.3838 mL | |
| 50 mM | 0.0763 mL | 0.3814 mL | 0.7628 mL | 1.9070 mL | |
| 60 mM | 0.0636 mL | 0.3178 mL | 0.6357 mL | 1.5892 mL | |
| 80 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1919 mL | |
| 100 mM | 0.0381 mL | 0.1907 mL | 0.3814 mL | 0.9535 mL |
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