1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. P-gp inhibitor 4

P-gp inhibitor 4 

Cat. No.: HY-146391
Handling Instructions

P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells.

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

P-gp inhibitor 4 Chemical Structure

P-gp inhibitor 4 Chemical Structure

CAS No. : 2652001-05-1

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Description

P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells[1].

IC50 & Target

EC50: 94 nM (P-glycoprotein)[1]

In Vitro

P-gp inhibitor 4 (Compound 8b) (0-1 μM, 48 h) significantly increases the cytotoxic effect of antineoplastic drug with co-administration[1].
P-gp inhibitor 4 does not alter the physiological properties of Caco-2 cells barrier model[1].
P-gp inhibitor 4 selectively reduces the activity of P-gp and increases the transport of multiple P-gp substrates across gastro-intestinal barrier[1].

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

Cell Proliferation Assay[1]

Cell Line: MDCK-MDR1
Concentration: 100 nM, 500 nM and 1 μM
Incubation Time: 48 h
Result: Showed no cytotoxicity. Significantly increased the cytotoxic effect of antineoplastic drug.

Cell Viability Assay[1]

Cell Line: Caco-2 cells
Concentration: 0.1 nM-100 µM
Incubation Time: 72 h
Result: Displayed a dose-dependence cytotoxicity that was significant at ≥ 10 μM concentration. Did not reduce cell viability at 100 nM.
Molecular Weight

714.85

Formula

C38H38N2O8S2

CAS No.
SMILES

COC1=CC=C(C=C1)S(=O)(N(S(=O)(C2=CC=C(C=C2)OC)=O)C3=CC=C(C=C3)C4=CC=C(C=C4)CN5CCC6=CC(OC)=C(C=C6C5)OC)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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P-gp inhibitor 4
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HY-146391
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