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Rislenemdaz mesylate

Chemical Structure : Rislenemdaz mesylate

CAS No.: 1893392-76-1

Rislenemdaz mesylate (MK 0657;CERC 301)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 454.517
Formula C20H27FN4O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-methylbenzyl (3S,4R)-3-fluoro-4-((pyrimidin-2-ylamino)methyl)piperidine-1-carboxylate mesylate

References

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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