Laniquidar
Based on 1 Customer Validation
Laniquidar is a non-competitive P-gp inhibitor with an IC50 of 0.51 μM. Laniquidar binds to the P-gp transporter with high affinity and exhibits low activity as a substrate. Laniquidar is applicable to epilepsy-related research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.86%
- No. CAS: 197509-46-9
- Fòrmula: C37H36N4O3
- Peso molecular:584.71
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Almacenamiento: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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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
Actividad biológica
IC50: 0.51 μM (P-glycoprotein)[1]
Laniquidar potently inhibits purified P-glycoprotein with an IC50 of 0.51 μM, acts primarily as an inhibitor rather than a substrate, and has higher P-gp binding affinity than verapamil[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:Wistar rats[1]
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Dosage:20 MBq; 100 MBq (metabolic stability)
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Administration:i.v.; single dose
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Result:Showed relatively high peripheral organ uptake in lung, liver, spleen, and kidney, with 30-minute %ID/g values of 4.49 (lung), 2.10 (liver), 1.08 (kidney), and 0.51 (heart).
Exhibited rapid blood clearance, with %ID/g below 0.11 by 5 minutes post-injection.
Demonstrated low cerebral uptake across all dissected brain regions, with relatively constant %ID/g from 5 to 60 minutes except for the olfactory bulb, which showed steadily increasing uptake.
Increased cerebral uptake significantly with cyclosporine A pretreatment, with cyclosporine A/normal ratios of 7.87 (cerebellum), 5.80 (hippocampus), 8.94 (cortex), and 7.89 (striatum) at 30 minutes post-injection.
Showed no significant effect on cerebral uptake with valspodar pretreatment compared to controls.
Had 68.0% of plasma radioactivity corresponding to parent [11C]laniquidar, with 31.5% as polar radioactive metabolites at 30 minutes post-injection.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 197509-46-9
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Appearance Solid
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Peso molecular 584.71
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Fòrmula C37H36N4O3
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Color White to off-white
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SMILES
O=C(C1=CN=C2/C(C3=C(CCN21)C=CC=C3)=C4CCN(CC\4)CCC5=CC=C(C=C5)OCC6=NC7=C(C=C6)C=CC=C7)OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 10 mg/mL (17.10 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. 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)
Pureza y Documentación
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Ficha de datos (272 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 |
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| DMSO | 1 mM | 1.7102 mL | 8.5512 mL | 17.1025 mL | 42.7562 mL |
| 5 mM | 0.3420 mL | 1.7102 mL | 3.4205 mL | 8.5512 mL | |
| 10 mM | 0.1710 mL | 0.8551 mL | 1.7102 mL | 4.2756 mL | |
| 15 mM | 0.1140 mL | 0.5701 mL | 1.1402 mL | 2.8504 mL |
Laniquidar Related Classifications
HY-132189 Related Classifications
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