Date published: 2025-12-5

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Mdr-1 Inhibitors

Mdr-1 inhibitors, also known as multidrug resistance protein 1 inhibitors, belong to a significant class of agents designed to modulate cellular efflux mechanisms. These inhibitors primarily target the multidrug resistance protein 1 (MDR-1) which is a transmembrane protein belonging to the ATP-binding cassette (ABC) transporter family. These transporters are integral in facilitating the efflux of a diverse array of substrates from within the cell to the extracellular environment. What sets Mdr-1 inhibitors apart is their role in impeding the function of the MDR-1 protein, effectively blocking its ability to pump out substrates from the cell. This interference with the transport function results from the interaction of the inhibitors with specific binding sites on the MDR-1 protein. This class of compounds encompasses a range of chemical structures, each with distinct properties governing their affinity for the MDR-1 binding sites. Structurally, Mdr-1 inhibitors exhibit considerable variability, reflecting the diverse chemical entities that constitute this class. Some common structural features include aromatic rings, heterocyclic moieties, and hydrophobic regions that facilitate interaction with the hydrophobic binding sites of MDR-1. These inhibitors act by competing for the same binding sites that substrates would typically occupy during the efflux process.

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Items 1 to 10 of 21 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

PSC 833

121584-18-7sc-361298
sc-361298A
sc-361298B
sc-361298C
sc-361298D
1 mg
10 mg
50 mg
100 mg
1 g
$213.00
$724.00
$2522.00
$4253.00
$26884.00
12
(1)

PSC-833 is a non-immunosuppressive cyclosporine derivative that inhibits MDR-1 by blocking drug efflux through P-glycoprotein.

Verapamil

52-53-9sc-507373
1 g
$367.00
(0)

Verapamil is a calcium channel blocker that can inhibit MDR-1 by blocking the efflux of drugs through P-glycoprotein, thus increasing intracellular drug levels.

MK-571

115103-85-0sc-201340
sc-201340A
5 mg
25 mg
$107.00
$413.00
8
(2)

MK-571 functions as a multidrug resistance (MDR) modulator by inhibiting the activity of the Mdr-1 transporter. It engages in specific binding interactions that alter the conformational dynamics of the transporter, effectively blocking the efflux of various substrates. This modulation can lead to increased intracellular concentrations of co-administered compounds, thereby influencing their pharmacokinetics and bioavailability. Its unique structural features allow for selective inhibition, impacting cellular transport mechanisms.

JS-2190

sc-221784
5 mg
$170.00
(0)

JS-2190 acts as a multidrug resistance (MDR) modulator by selectively interacting with the Mdr-1 transporter. Its unique molecular structure facilitates specific binding that disrupts the transporter's normal function, leading to altered substrate efflux dynamics. This interaction enhances the retention of various compounds within cells, significantly affecting their distribution and metabolic pathways. The compound's distinct kinetic profile allows for targeted modulation of cellular transport processes.

Cyclosporin A

59865-13-3sc-3503
sc-3503-CW
sc-3503A
sc-3503B
sc-3503C
sc-3503D
100 mg
100 mg
500 mg
10 g
25 g
100 g
$62.00
$90.00
$299.00
$475.00
$1015.00
$2099.00
69
(5)

Cyclosporine A is an immunosuppressive drug that inhibits MDR-1 by binding to P-glycoprotein and preventing its drug efflux activity.

Zosuquidar trihydrochloride

167465-36-3sc-364314
sc-364314A
5 mg
10 mg
$138.00
$330.00
2
(0)

Zosuquidar trihydrochloride functions as a potent modulator of the Mdr-1 transporter, exhibiting a unique affinity for its binding sites. This compound alters the conformational dynamics of the transporter, impacting substrate recognition and translocation efficiency. Its specific interactions can lead to a pronounced alteration in cellular efflux mechanisms, thereby influencing the intracellular accumulation of various substrates. The compound's behavior is characterized by distinct kinetic properties that facilitate nuanced control over transport activity.

Sipholenol A

78518-73-7sc-222313
100 µg
$200.00
(0)

Sipholenol A exhibits a unique mechanism of action as a modulator of the Mdr-1 transporter, characterized by its ability to stabilize specific conformations of the protein. This stabilization alters the transporter's affinity for various substrates, impacting the kinetics of efflux processes. Its distinctive hydrophobic regions facilitate interactions with membrane lipids, potentially influencing membrane fluidity and transport efficiency. The compound's intricate molecular architecture plays a crucial role in its transport modulation capabilities.

Matairesinol

580-72-3sc-205379
sc-205379A
sc-205379B
1 mg
5 mg
25 mg
$56.00
$170.00
$795.00
(0)

Matairesinol acts as a selective modulator of the Mdr-1 transporter, engaging in specific molecular interactions that enhance its binding affinity. This compound influences the transporter's conformational states, thereby affecting substrate specificity and transport kinetics. Its unique structural features allow for tailored interactions with lipid membranes, potentially altering permeability and efflux rates. The compound's distinct behavior in cellular environments underscores its role in modulating transport dynamics.

P-Glycoprotein Inhibitor, C-4

sc-222109
10 mg
$430.00
(0)

P-Glycoprotein Inhibitor, C-4 operates through a distinctive binding affinity that disrupts the normal function of the Mdr-1 transporter. By engaging in specific hydrogen bonding and hydrophobic interactions, it alters the conformational dynamics of the protein, leading to a reduced substrate translocation rate. This compound's unique structural features enhance its ability to interfere with the ATPase activity of the transporter, thereby modulating its efflux capacity and influencing cellular accumulation of various compounds.

Reversin 121

174630-04-7sc-205969
5 mg
$300.00
2
(1)

Reversin 121 exhibits a remarkable ability to modulate the Mdr-1 transporter by engaging in selective molecular interactions that stabilize its inactive conformation. This compound disrupts the ATP hydrolysis cycle, effectively diminishing the energy-dependent efflux mechanism. Its unique structural motifs facilitate specific van der Waals forces and electrostatic interactions, leading to altered substrate affinity and a significant impact on the transport kinetics of various substrates.