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 11 to 20 of 21 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Pyrimethamine-d3

1189936-99-9sc-219678
1 mg
$330.00
(0)

Pyrimethamine-d3 exhibits a remarkable ability to modulate the Mdr-1 transporter by engaging in selective molecular interactions that facilitate its transport dynamics. The compound's isotopic labeling enhances its detection in biochemical assays, allowing for precise tracking of its influence on transporter activity. Its unique structural features promote specific electrostatic interactions and steric effects, which can significantly impact the kinetics of substrate efflux and the overall transport mechanism.

Pyrimethamine

58-14-0sc-208190
sc-208190A
sc-208190B
1 g
5 g
25 g
$78.00
$233.00
$809.00
5
(0)

Pyrimethamine demonstrates intriguing behavior as an Mdr-1 modulator through its ability to alter membrane permeability and influence substrate binding affinities. Its unique structural conformation allows for specific hydrogen bonding and hydrophobic interactions with the transporter, potentially affecting conformational changes. The compound's kinetic profile reveals a nuanced interplay between competitive inhibition and allosteric modulation, which can lead to variations in transport efficiency and substrate specificity.

Niguldipine hydrochloride

113317-61-6sc-201471
sc-201471A
10 mg
50 mg
$79.00
$318.00
(0)

Niguldipine hydrochloride exhibits distinctive characteristics as an Mdr-1 modulator, primarily through its capacity to interact with lipid bilayers and alter membrane dynamics. Its unique stereochemistry facilitates specific electrostatic interactions with the transporter, influencing its conformational states. The compound's reaction kinetics suggest a complex mechanism involving both competitive and non-competitive inhibition, which may impact the transporter's substrate recognition and translocation efficiency.

CP 100356 hydrochloride

142716-85-6sc-361154
sc-361154A
10 mg
50 mg
$370.00
$1100.00
(0)

CP 100356 hydrochloride demonstrates unique properties as an Mdr-1 modulator, characterized by its ability to disrupt protein-lipid interactions within cellular membranes. This compound engages in specific hydrogen bonding and hydrophobic interactions, which can stabilize or destabilize the transporter’s structure. Its kinetic profile indicates a nuanced interplay of binding affinities, potentially leading to altered substrate specificity and transport dynamics, thereby influencing cellular efflux mechanisms.

Reversan

313397-13-6sc-296262
sc-296262A
10 mg
50 mg
$185.00
$781.00
3
(0)

Reversan acts as a potent Mdr-1 modulator, exhibiting distinctive interactions with membrane proteins that alter their conformational states. It engages in specific electrostatic and van der Waals interactions, which can enhance or inhibit the activity of the transporter. The compound's unique reaction kinetics suggest a complex binding mechanism, potentially affecting the transporter's affinity for various substrates and modifying efflux pathways in cellular environments.

PGP-4008

365565-02-2sc-222152
sc-222152A
2 mg
10 mg
$107.00
$349.00
1
(1)

PGP-4008 functions as a notable Mdr-1 modulator, characterized by its ability to disrupt typical substrate translocation through intricate molecular interactions. It engages in selective hydrogen bonding and hydrophobic interactions with the transporter, influencing its structural dynamics. The compound's unique kinetic profile indicates a multi-step binding process, which may alter the transporter's substrate specificity and efflux efficiency, thereby impacting cellular transport mechanisms.

Elacridar

143664-11-3sc-207613A
sc-207613
sc-207613B
sc-207613C
sc-207613D
5 mg
10 mg
50 mg
100 mg
1 g
$96.00
$111.00
$403.00
$515.00
$2555.00
19
(1)

Elacridar inhibits MDR-1 by binding to P-glycoprotein and preventing drug efflux, enhancing drug delivery to target tissues.

8-Isopentenylnaringenin

68682-02-0sc-221146
5 mg
$326.00
(0)

8-Isopentenylnaringenin acts as a significant Mdr-1 modulator, exhibiting a unique capacity to alter transporter conformation through specific ligand-receptor interactions. Its distinct molecular architecture facilitates enhanced binding affinity, leading to competitive inhibition of substrate transport. The compound's influence on the allosteric sites of the transporter suggests a complex interplay of steric and electronic effects, potentially reshaping the efflux pathways and modulating cellular permeability.

Vismodegib

879085-55-9sc-396759
sc-396759A
10 mg
25 mg
$80.00
$96.00
1
(0)

Vismodegib functions as a notable Mdr-1 modulator, characterized by its ability to disrupt the normal transport dynamics of substrates. Its unique structural features enable it to engage in specific interactions with the transporter, promoting conformational changes that hinder substrate efflux. This compound's kinetic profile indicates a selective binding mechanism, influencing the transporter's activity and potentially altering the cellular microenvironment through modulation of efflux efficiency.

Pyrimethamine Biotin

sc-219677
10 mg
$360.00
(0)

Pyrimethamine Biotin demonstrates a distinctive capacity to influence the Mdr-1 transporter through intricate binding dynamics that promote conformational changes. This compound interacts with key amino acid residues, enhancing the stability of the transporter’s substrate-binding site. Its unique chemical structure allows for specific hydrogen bonding and hydrophobic interactions, which modulate the transport efficiency and alter the kinetics of substrate translocation across cellular membranes.