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.
For research use only. We do not sell to patients.
- Formula: C21H27NO4
- Molecular Weight:357.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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
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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. Further protocols information, click here.
Chemical Information
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Molecular Weight 357.44
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Formula C21H27NO4
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SMILES
COC1=CC(CCN(CCCOC2=CC=CC(OC)=C2)C3)=C3C=C1OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)