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Rislenemdaz hydrochloride

Chemical Structure : Rislenemdaz hydrochloride

CAS No.: 808733-06-4

Rislenemdaz hydrochloride (MK 0657;CERC 301)

Catalog No.: PC-61909Not 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 394.875
    Formula C19H24ClFN4O2
    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 hydrochloride

    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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