1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. Laniquidar

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.

For research use only. We do not sell to patients.

Laniquidar

Laniquidar Chemical Structure

CAS No. : 197509-46-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target

IC50: 0.51 μM (P-glycoprotein)[1]

In Vitro

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.

In Vivo

11C]laniquidar (20-100 MBq; i.v.; single dose) shows low cerebral uptake in healthy Wistar rats, which is significantly increased by cyclosporine A pretreatment but unaffected by valspodar, and exhibits relatively low in vivo plasma metabolism[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats[1]
Dosage: 20 MBq; 100 MBq (metabolic stability)
Administration: i.v.; single dose
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.
Clinical Trial
Molecular Weight

584.71

Formula

C37H36N4O3

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7102 mL 8.5512 mL 17.1025 mL
5 mM 0.3420 mL 1.7102 mL 3.4205 mL
View the 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.

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Purity & Documentation
References

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Laniquidar
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HY-132189
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