Rislenemdaz (MK-0657) (Synonyms: MK-0657; CERC-301) |
Catalog No.GC30835 |
Rislenemdaz (MK-0657) (CERC-301) es un antagonista de la subunidad 2B (GluN2B) del receptor de N-metil-D-aspartato (NMDA) selectivo y biodisponible por vÍa oral con Ki y IC 50 de 8,1 nM y 3,6 nM, respectivamente.
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Cas No.: 808732-98-1
Sample solution is provided at 25 µL, 10mM.
Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
Rislenemdaz (CERC-301) inhibits calcium influx into agonist-stimulating NMDA-GluN1a/GluN2B L(tk-) cells with an IC50 of 3.6 nM. Rislenemdaz exhibits at least 1000× selectivity for the GluN2B receptor versus all targets tested, including the hERG potassium channel. Rislenemdaz also exhibits minimal activity against sigma-type receptors at 10 uM[1].
Rislenemdaz (CERC-301) (1, 3, 10, and 30 mg/kg) significantly decreases immobility frequency (P
[1]. Rachel Garner, et al. Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N‐methyl‐D‐aspartate receptor antagonist. Pharmacol Res Perspect. 2015 Dec; 3(6): e00198.
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