LysRs-IN-2
Based on 1 publication(s) in Google Scholar
LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively.
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- Reinheit: 99.92%
- CAS. Nr.: 2170696-76-9
- Formel: C17H16F3NO4
- Molecular Weight:355.31
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Speicherung:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LysRs-IN-2
More
Biologische Aktivität
IC50: 0.015 μM (PfKRS), 0.13 μM (CpKRS)[1]
LysRs-IN-2 is active against whole-cell bloodstream P. falciparum 3D7 (EC50=0.27 μM), HsKRS (IC50=1.8 μM), HepG2 cells (EC50=49 μM), and Cryptosporidium parvum (EC50=2.5 µM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine P. falciparum NODscidIL2Rγnull (SCID) model[1]
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Dosage:1.5 mg/kg
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Administration:Orally once a day for 4 days
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Result:Reduced parasitemia by 90% in the malaria SCID mouse model.
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Animal Model:NOD SCID gamma and INF-γ–knockout mouse models (Cryptosporidium mouse models)[1]
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Dosage:20 mg/kg
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Administration:Orally once a day for 7 days
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Result:Reduced parasite shedding below detection level, and this reduction was sustained for 3 wk after treatment had stopped in INF-γ-knockout mice. Dosed orally at a concentration of 20 mg/kg once a day for 7 days showed 96% reduction of parasite shedding comparable to paromomycin in NOD SCID gamma mice.
Chemical Information
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CAS. Nr. 2170696-76-9
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Appearance Solid
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Molecular Weight 355.31
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Formel C17H16F3NO4
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Color White to off-white
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SMILES
FC1=CC=C(OC(C(NCC2(O)CCC(F)(F)CC2)=O)=CC3=O)C3=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Translation inhibition efficacy does not determine the Plasmodium berghei liver stage antiplasmodial efficacy of protein synthesis inhibitors. [Abstract]2023 Dec 7:2023.12.07.570699. PMID: 38106175
Lösungsmittel & Löslichkeit
DMSO : ≥ 60 mg/mL (168.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (5.85 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.5 mg/mL (4.22 mM); Clear solution
This protocol yields a clear solution of ≥ 1.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 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.
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.
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8144 mL | 14.0722 mL | 28.1444 mL | 70.3611 mL |
| 5 mM | 0.5629 mL | 2.8144 mL | 5.6289 mL | 14.0722 mL | |
| 10 mM | 0.2814 mL | 1.4072 mL | 2.8144 mL | 7.0361 mL | |
| 15 mM | 0.1876 mL | 0.9381 mL | 1.8763 mL | 4.6907 mL | |
| 20 mM | 0.1407 mL | 0.7036 mL | 1.4072 mL | 3.5181 mL | |
| 25 mM | 0.1126 mL | 0.5629 mL | 1.1258 mL | 2.8144 mL | |
| 30 mM | 0.0938 mL | 0.4691 mL | 0.9381 mL | 2.3454 mL | |
| 40 mM | 0.0704 mL | 0.3518 mL | 0.7036 mL | 1.7590 mL | |
| 50 mM | 0.0563 mL | 0.2814 mL | 0.5629 mL | 1.4072 mL | |
| 60 mM | 0.0469 mL | 0.2345 mL | 0.4691 mL | 1.1727 mL | |
| 80 mM | 0.0352 mL | 0.1759 mL | 0.3518 mL | 0.8795 mL | |
| 100 mM | 0.0281 mL | 0.1407 mL | 0.2814 mL | 0.7036 mL |
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