P-gp-IN-37
P-gp-IN-37 is a ligand of P-glycoprotein (P-gp), with an EC50 value of 1.8 μM. P-gp-IN-37 stabilizes the inward-facing conformation of P-gp through hydrogen bonding and π-stacking interactions, and can be used as a PET radiotracer for imaging the function and expression of P-gp. P-gp-IN-37 is applied in the research of heart failure.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C21H27NO4
- Peso molecular:357.44
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
IC50 & Target
[1]|
P-gp 1.8 μM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDCK-MDR1 | EC50 |
1.8 μM
|
Modulation of P-glycoprotein (P-gp) activity in MDCK-MDR1 cells assessed via Calcein-AM Transport Assay with 30 min pre-incubation with cells followed by 30 min incubation with Calcein-AM, measured by fluorescence intensity.
Modulation of P-glycoprotein (P-gp) activity in MDCK-MDR1 cells assessed via Calcein-AM Transport Assay with 30 min pre-incubation with cells followed by 30 min incubation with Calcein-AM, measured by fluorescence intensity.
|
42597856 |
In Vitro
P-gp-IN-37 (compound 2c) (0.1-100 μM; 30 min pre-incubation with cells; 30 min incubation with Calcein-AM (HY-D0041)) potently modulates P-gp activity in MDCK-MDR1 cells, with an EC50 value of 1.8 μM[1].
P-gp-IN-37 (500 ns production run) stabilizes the inward-closed conformation of human P-gp through sustained intramolecular interactions and protein-ligand interactions, thereby reducing its large-scale domain motion and conformational flexibility[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Peso molecular 357.44
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Fòrmula C21H27NO4
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SMILES
COC1=CC(CCN(CCCOC2=CC=CC(OC)=C2)C3)=C3C=C1OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)