Rislenemdaz

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、口服生物可利用的脑渗透性、NR2B 选择性 NMDA 受体 (GluN2B) 拮抗剂，Ki 和 IC 50 分别为 8.1 nM 和 3.6 nM。

A potent, orally bioavailable brain‐penetrant, NR2B-selective NMDA receptor (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM respectively, with no off-target activity; inhibits calcium influx into agonist‐stimulated NMDA‐GluN1a/GluN2B L(tk‐) cells with IC50 of 3.6 nM, with no effect on GluN2A up to 30 uM; significantly decreases immobility frequency and increases swimming behavior in acute depression models.Depression Phase 1 Clinical.

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.

Rislenemdaz (CERC-301) (1, 3, 10, and 30 mg/kg) significantly decreases immobility frequency (P<0.001) and significantly increases swimming behavior (P<0.01 for 1, 3, and 30 mg/kg; P<0.05 for 10 mg/kg) compare to the vehicle control.Rislenemdaz plasma levels are approximately 15, 120, 390, 1420, 4700, and 14,110 nM (0.015, 0.120, 0.390, 1.42, 4.7, and 14.11 uM) at the time of sampling, corresponding to approximately 5, 29, 56, 83, 94, and 98% RO, respectively, in rats. The ED50 for increaing in frequency of swimming and decreasing in immobility are ~0.3 and 0.7 mg/kg, respectively, corresponding to RO of ~30 and 50%. Rislenemdaz (1, 3, 10, and 30 mg/kg) significantly increases total distance traveling (P<0.01 for 1 mg/kg; P<0.001 for 3, 10, and 30 mg/kg) compare to vehicle control over the 60 min test.

MK-0657 | CERC-301 | MK 0657 | MK0657 | CERC 301 | CERC301

Membrane Transporter/Ion Channel

iGluR

iGluR

Neurological Disease

Depression

808732-98-1

358.417

C19H23FN4O2

>98% (HPLC)

DMSO : 150 mg/mL 418.52 mM

CC1=CC=C(C=C1)COC(=O)N2CCC(C(C2)F)CNC3=NC=CC=N3

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(-20℃)

With Ice Pack

≥ 2 years