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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-Rislenemdaz
Rislenemdaz

Chemical Structure : Rislenemdaz

CAS No.: 808732-98-1

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Rislenemdaz (MK-0657;CERC-301;MK 0657;MK0657;CERC 301;CERC301)

货号: PC-42691Not For Human Use, Lab Use Only.

Rislenemdaz (MK-0657, CERC-301) is 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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Rislenemdaz (MK-0657, CERC-301) is 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.
Rislenemdaz (MK-0657, CERC-301)  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.
Rislenemdaz (MK-0657, CERC-301)  significantly decreases immobility frequency and increases swimming behavior in acute depression models.

物理化学性质&存储条件

分子量 358.417
分子式 C19H23FN4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(4-Methylphenyl)methyl (3S,4R)-3-fluoro-4-[(2-pyrimidinylamino)methyl]-1-piperidinecarboxylate

参考文献

1. Addy C, et al. J Clin Pharmacol. 2009 Jul;49(7):856-64.

2. Ibrahim L, et al. J Clin Psychopharmacol. 2012 Aug;32(4):551-7.

3. Garner R, et al. Pharmacol Res Perspect. 2015 Dec 23;3(6):e00198.

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