PGP Activators
PGP activators encompass a diverse group of chemicals that modulate the activity of P-glycoprotein (PGP), a vital efflux transporter involved in cellular drug disposition. Verapamil, a calcium channel blocker, potentially activates PGP by influencing intracellular calcium levels. The interaction of Verapamil with calcium channels initiates signaling cascades that impact PGP activity, altering drug efflux dynamics. Rifampicin, an antibiotic, induces PGP expression through the activation of nuclear receptors like pregnane X receptor (PXR). This activation leads to increased transcription of PGP-encoding genes, enhancing PGP activity and influencing drug efflux patterns. Curcumin, a polyphenolic compound, potentially activates PGP by modulating NF-κB signaling. Its anti-inflammatory effects may contribute to NF-κB inhibition, indirectly influencing PGP and enhancing its activity in specific cellular contexts.
Probenecid, an organic anion transporter inhibitor, indirectly affects PGP by reducing its efflux substrates. This leads to increased intracellular concentrations of PGP substrates, influencing PGP activity and contributing to altered drug efflux patterns. Tamoxifen, a selective estrogen receptor modulator, exhibits dual actions as an antagonist on estrogen receptors and a potential activator of PGP through interaction with nuclear receptors like PXR. This modulation can lead to increased PGP expression and activity. Ketoconazole, an antifungal agent, may activate PGP through the inhibition of cytochrome P450 enzymes. By modulating these enzymes, Ketoconazole indirectly influences PGP activity, altering the metabolism of PGP substrates. St. John's Wort, a herbal remedy, may induce PGP expression through the activation of nuclear receptors like PXR, leading to increased transcription of PGP-encoding genes and altered PGP expression and activity. In summary, the diverse mechanisms by which these chemicals potentially activate PGP provide a comprehensive framework for understanding the modulation of this essential efflux transporter in various cellular contexts.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Rifampicin | 13292-46-1 | sc-200910 sc-200910A sc-200910B sc-200910C | 1 g 5 g 100 g 250 g | $97.00 $328.00 $676.00 $1467.00 | 6 | |
Antibiotic known to induce PGP expression, possibly through activation of nuclear receptors like PXR, subsequently promoting PGP activity. The activation of PXR by Rifampicin initiates a cascade of events, including enhanced transcription of PGP-encoding genes. | ||||||
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $37.00 $69.00 $109.00 $218.00 $239.00 $879.00 $1968.00 | 47 | |
Polyphenolic compound with potential PGP-activating properties, possibly influencing PGP expression through modulation of NF-κB signaling. Curcumin's anti-inflammatory effects may contribute to NF-κB inhibition, indirectly affecting PGP and enhancing its activity in certain cellular contexts. | ||||||
Probenecid | 57-66-9 | sc-202773 sc-202773A sc-202773B sc-202773C | 1 g 5 g 25 g 100 g | $28.00 $39.00 $100.00 $277.00 | 28 | |
Organic anion transporter inhibitor that indirectly affects PGP by reducing its efflux substrates, leading to increased intracellular concentrations of PGP substrates. Probenecid's impact on transporter dynamics can influence PGP activity and contribute to altered drug efflux patterns. | ||||||
Tamoxifen | 10540-29-1 | sc-208414 | 2.5 g | $272.00 | 18 | |
Selective estrogen receptor modulator with dual actions, acting as an antagonist on estrogen receptors and potentially activating PGP through interaction with nuclear receptors, such as PXR. The modulation of PXR by Tamoxifen may lead to increased PGP expression and activity. | ||||||
Etoposide (VP-16) | 33419-42-0 | sc-3512B sc-3512 sc-3512A | 10 mg 100 mg 500 mg | $51.00 $231.00 $523.00 | 63 | |
Topoisomerase II inhibitor that induces PGP expression, possibly through the activation of stress response pathways. Etoposide's impact on cellular stress can trigger signaling cascades leading to increased PGP expression, contributing to altered drug efflux dynamics. | ||||||
Quercetin | 117-39-5 | sc-206089 sc-206089A sc-206089E sc-206089C sc-206089D sc-206089B | 100 mg 500 mg 100 g 250 g 1 kg 25 g | $11.00 $17.00 $110.00 $250.00 $936.00 $50.00 | 33 | |
Flavonoid compound with potential PGP-activating properties, potentially influencing PGP expression through modulation of NF-κB signaling. Quercetin's anti-inflammatory effects may contribute to NF-κB inhibition, indirectly affecting PGP and enhancing its activity in specific cellular contexts. | ||||||
Omeprazole | 73590-58-6 | sc-202265 | 50 mg | $67.00 | 4 | |
Proton pump inhibitor that potentially activates PGP by modulating intracellular pH levels. Omeprazole's impact on cellular acidity can influence PGP activity, leading to altered drug efflux patterns and potential changes in the cellular response to PGP substrates. | ||||||
Nifedipine | 21829-25-4 | sc-3589 sc-3589A | 1 g 5 g | $59.00 $173.00 | 15 | |
Calcium channel blocker that may activate PGP by modulating intracellular calcium levels. Similar to Verapamil, Nifedipine's interaction with calcium channels can influence cellular signaling cascades, leading to changes in PGP activity. | ||||||