Galeflaprit
Based on 1 Customer Validation
Galeflaprit (LXE408) is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. Galeflaprit has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. Galeflaprit has a low propensity to cross the blood brain barrier. Galeflaprit has the potential for visceral leishmaniasis (VL) research.
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- Pureza: 99.75%
- No. CAS: 1799330-15-6
- Fòrmula: C23H18FN7O2
- Peso molecular:443.43
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Leishmania |
Galeflaprit (LXE408) (compound 1) can occupy the pocket as a ternary complex with the proteasome. Galeflaprit shows no inhibition of the hERG channel (IC50>30 μM) in a manual patch clamp assay. Galeflaprit has a low propensity to cross the blood brain barrier (brain/plasma AUC ratio=0.03 in mice)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Galeflaprit (1, 3, 10, 20 mg/kg; p.o.; b.i.d.; for 10 days) effects robust healing of parasite-induced skin lesions at the base of the tail in BALB/c mice infected with L. major[1].
Galeflaprit (5 mg/kg IV and 20 mg/kg PO) has a T1/2 of 3.3 hours for mouse. Galeflaprit (3 mg/kg IV and 10 mg/kg PO) has a T1/2 of 3.8 hours, a CL of 2.1 mL/min kg, and a Vss of 0.53 L/kg for male Sprague-Dawley rat[1].
Galeflaprit (0.3 mg/kg IV and 1.0 mg/kg PO) has a T1/2 of 3.8 hours for male beagle dog. Galeflaprit (0.3 mg/kg IV and 10 mg/kg PO) has a T1/2 of 9.7 hours for male cynomolgus monkey[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (6-8 weeks old) infected with L. donovani[1]
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Dosage:0.3, 1, 3, 10 mg/kg
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Administration:PO; twice daily for 8 days
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Result:Led to a 95% and >99.84% reduction of parasite burden in the liver at 1 mg/kg and 10 mg/kg.
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Animal Model:Balb/C mice[1]
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Dosage:5 mg/kg IV and 20 mg/kg PO (Pharmacokinetic Analysis)
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Administration:IV or PO
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Result:Had a T1/2 of 3.3 hours, a CL of 2.3 mL/min•kg, and a Vss of 0.63 L/kg for mouse.
Chemical Information
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No. CAS 1799330-15-6
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Appearance Solid
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Peso molecular 443.43
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Fòrmula C23H18FN7O2
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Color Off-white to light yellow
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SMILES
O=C(C1=C(C)N=C(C)O1)NC2=CC=C(F)C(C3=NN4C=C(C5=NC=CC=C5C)C=NC4=N3)=C2
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Synonyms
LXE408
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 16.67 mg/mL (37.59 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: ≥ 0.62 mg/mL (1.40 mM); Clear solution
This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 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: ≥ 0.62 mg/mL (1.40 mM); Clear solution
This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 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.
Pureza y Documentación
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Ficha de datos (286 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)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.2551 mL | 11.2757 mL | 22.5515 mL | 56.3787 mL |
| 5 mM | 0.4510 mL | 2.2551 mL | 4.5103 mL | 11.2757 mL | |
| 10 mM | 0.2255 mL | 1.1276 mL | 2.2551 mL | 5.6379 mL | |
| 15 mM | 0.1503 mL | 0.7517 mL | 1.5034 mL | 3.7586 mL | |
| 20 mM | 0.1128 mL | 0.5638 mL | 1.1276 mL | 2.8189 mL | |
| 25 mM | 0.0902 mL | 0.4510 mL | 0.9021 mL | 2.2551 mL | |
| 30 mM | 0.0752 mL | 0.3759 mL | 0.7517 mL | 1.8793 mL |
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