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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.86%
- CAS 番号: 197509-46-9
- 分子式: C37H36N4O3
- 分子量:584.71
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Tariquidar (Standard)P-gp Inhibitor
生物活性
製品説明
IC50 & Target
IC50: 0.51 μM (P-glycoprotein)[1]
体外実験
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.
体内実験
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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 197509-46-9
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性状 Solid
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分子量 584.71
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 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 関連分類
HY-132189 関連分類
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