NMQ/N-methyl-quinidine - MDR1/P-gp Substrate

Product Cell Line Transporter Technology Membrane Type Probe Substrate Read Out Reference Inhibitor Positive Control Dynamic Range
SB NMQ 5 mg/10 mg/50 mg/100 mg/500 mg/1g MDR1/P-gp

Description

SOLVO Biotechnology offers NMQ as a potent MDR1 membrane transporter substrate. 

N-methyl-quinidine (NMQ), a low permeability amphipathic monoquaternary molecule, is an excellent cationic model compound. NMQ was shown to be actively transported by human MDR1/P-gp and rat Mdr1b efflux transporters (Hooiveld et al, 2002), as well as by the human OATP-A (OATP1A2) uptake transporter (van Montfoort et al, 1999). The apparent Km values were 15 μM, 20 μM and 26 μM for the MDR1, Mdr1b and OATP-A transporters, respectively.

Kinetic parameters of human MDR1- and rat Mdr1b-mediated NMQ transport into transporter containing and control membrane vesicles have been validated using SOLVO membrane preparations (SB-MDR1-K-VT, SB-K-CTRL, SB-ratMdr1b-Sf9-VT, SB-defPgp-Sf9-VT). The human MDR1 transporter was expressed in mammalian cells (MDR1-K), while the rat Mdr1b transporter was expressed in Sf9 cells using a baculoviral infection system (ratMdr1b-Sf9).

Learn more about N-methyl-quinidine (NMQ).

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