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
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M.Wt
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454.517
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Formula
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C20H27FN4O5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-methylbenzyl (3S,4R)-3-fluoro-4-((pyrimidin-2-ylamino)methyl)piperidine-1-carboxylate mesylate
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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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