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Rislenemdaz mesylate

CAS No. 1893392-76-1

Rislenemdaz mesylate( MK 0657 | CERC 301 )

Catalog No. M12971 CAS No. 1893392-76-1

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.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Rislenemdaz mesylate
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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; 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; significantly decreases immobility frequency and increases swimming behavior in acute depression models.Depression Phase 2 Clinical.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    MK 0657 | CERC 301
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    iGluR
  • Recptor
    iGluR
  • Research Area
    Neurological Disease
  • Indication
    Depression

Chemical Information

  • CAS Number
    1893392-76-1
  • Formula Weight
    454.517
  • Molecular Formula
    C20H27FN4O5S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    ——
  • Chemical Name
    4-methylbenzyl (3S,4R)-3-fluoro-4-((pyrimidin-2-ylamino)methyl)piperidine-1-carboxylate mesylate

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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