Rislenemdaz mesylate |CAS:1893392-76-1 Probechem Biochemicals

Chemical Structure : Rislenemdaz mesylate

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Rislenemdaz mesylate (MK 0657;CERC 301)

货号: PC-61911Not For Human Use, Lab Use Only.

Rislenemdaz mesylate (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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生物&药学活性

Rislenemdaz mesylate (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 mesylate (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 mesylate (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	454.517
分子式	C20H27FN4O5S
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-methylbenzyl (3S,4R)-3-fluoro-4-((pyrimidin-2-ylamino)methyl)piperidine-1-carboxylate mesylate

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.

Rislenemdaz mesylate (MK 0657;CERC 301)

生物&药学活性

物理化学性质&存储条件

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Rislenemdaz mesylate (MK 0657;CERC 301)

生物&药学活性

物理化学性质&存储条件

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