LasR antagonist-2
Based on 1 Customer Validation
LasR antagonist-2 is a LasR competitive antagonist and quorum sensing inhibitor, with a Kd value of 7.04 μM against LasR of Pseudomonas aeruginosa. LasR antagonist-2 reduces the production of virulence factors including elastase (elastase), pyocyanin (pyocyanin) and rhamnolipid (rhamnolipid). LasR antagonist-2 inhibits bacterial (bacterial) swarming and swimming motility, and moderately suppresses biofilm formation. LasR antagonist-2 inhibits Pseudomonas aeruginosa infection in the greater wax moth larva model. Elastase-IN-3 can be used in studies related to Pseudomonas aeruginosa infection.
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- Pureté : 99.69%
- CAS No.: 15015-57-3
- Formule: C12H10O2S2
- Masse moléculaire:250.34
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Stockage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16-F1 | IC50 |
21.2 %
Compound: 6
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Cytotoxicity against mouse B16-F1 cells after 48 hrs by MTT assay
Cytotoxicity against mouse B16-F1 cells after 48 hrs by MTT assay
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[PMID: 19601648] |
In Vitro
LasR antagonist-2 (Compound 2i) (80 μg/mL; 12 h) potently inhibits quorum-sensing gene expression in the P. aeruginosa PAO1 reporter strain, with an inhibition rate of over 75% at a concentration of 80 μg/mL[1].
LasR antagonist-2 (80 μg/mL; 12-24 h) potently inhibits the production of elastase, pyocyanin and rhamnolipid in P. aeruginosa PAO1[1].
LasR antagonist-2 (80 μg/mL; 16 h) potently inhibits the swarming and swimming motility of P. aeruginosa PAO1 at a concentration of 80 μg/mL[1].
LasR antagonist-2 (80 μg/mL; 24 h) inhibits biofilm formation by P. aeruginosa PAO1 by 32%[1].
LasR antagonist-2 (80 μg/mL; 12 h) synergistically enhances the antibacterial activity of Ciprofloxacin (HY-B0356) and Tobramycin (HY-B0441) against P. aeruginosa PAO1[1].
LasR antagonist-2 (80 μg/mL; 6 h) downregulates the expression of key quorum-sensing genes in P. aeruginosa PAO1, thereby inhibiting the quorum-sensing pathway[1].
LasR antagonist-2 (10-2560 nM; 600 s contact time, 360 s dissociation time) directly interacts with the LasR protein of P. aeruginosa PAO1, with a KD value of 7.04 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:larvae (uniform size 20 mm, weight 200 mg, no gray pigmentation)[1]
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Dosage:80 μg/mL
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Administration:injection; concurrent with infection challenge
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Result:Increased larval survival rate to 90% at 72 hours post-infection.
Chemical Information
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CAS No. 15015-57-3
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Appearance Solid
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Masse moléculaire 250.34
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Formule C12H10O2S2
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Color Off-white to light yellow
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SMILES
OC(C=C1)=CC=C1SSC2=CC=C(O)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (199.73 mM; Need ultrasonic; 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 (stored under nitrogen). 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 (stored under nitrogen). 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (19.97 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Pureté et documentation
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Fiche technique (272 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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Instruction de manipulation (2659 KB)
Références
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 (stored under nitrogen). 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 | 3.9946 mL | 19.9728 mL | 39.9457 mL | 99.8642 mL |
| 5 mM | 0.7989 mL | 3.9946 mL | 7.9891 mL | 19.9728 mL | |
| 10 mM | 0.3995 mL | 1.9973 mL | 3.9946 mL | 9.9864 mL | |
| 15 mM | 0.2663 mL | 1.3315 mL | 2.6630 mL | 6.6576 mL | |
| 20 mM | 0.1997 mL | 0.9986 mL | 1.9973 mL | 4.9932 mL | |
| 25 mM | 0.1598 mL | 0.7989 mL | 1.5978 mL | 3.9946 mL | |
| 30 mM | 0.1332 mL | 0.6658 mL | 1.3315 mL | 3.3288 mL | |
| 40 mM | 0.0999 mL | 0.4993 mL | 0.9986 mL | 2.4966 mL | |
| 50 mM | 0.0799 mL | 0.3995 mL | 0.7989 mL | 1.9973 mL | |
| 60 mM | 0.0666 mL | 0.3329 mL | 0.6658 mL | 1.6644 mL | |
| 80 mM | 0.0499 mL | 0.2497 mL | 0.4993 mL | 1.2483 mL | |
| 100 mM | 0.0399 mL | 0.1997 mL | 0.3995 mL | 0.9986 mL |
LasR antagonist-2 Related Classifications
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