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Rislenemdaz
CAS No. 808732-98-1
Rislenemdaz( MK-0657 | CERC-301 | MK 0657 | MK0657 | CERC 301 | CERC301 )
Catalog No. M16023 CAS No. 808732-98-1
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)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 402 | Get Quote |
|
| 10MG | 593 | Get Quote |
|
| 25MG | 888 | Get Quote |
|
| 50MG | 1251 | Get Quote |
|
| 100MG | 1692 | Get Quote |
|
| 500MG | 3402 | Get Quote |
|
| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameRislenemdaz
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NoteResearch use only, not for human use.
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Brief DescriptionA 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.
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DescriptionA 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 1 Clinical.
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In VitroRislenemdaz (CERC-301) inhibits calcium influx into agonist-stimulating NMDA-GluN1a/GluN2B L(tk-) cells with an IC50 of 3.6 nM. Rislenemdaz exhibits at least 1000× selectivity for the GluN2B receptor versus all targets tested, including the hERG potassium channel. Rislenemdaz also exhibits minimal activity against sigma-type receptors at 10 uM.
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In VivoRislenemdaz (CERC-301) (1, 3, 10, and 30 mg/kg) significantly decreases immobility frequency (P<0.001) and significantly increases swimming behavior (P<0.01 for 1, 3, and 30 mg/kg; P<0.05 for 10 mg/kg) compare to the vehicle control.Rislenemdaz plasma levels are approximately 15, 120, 390, 1420, 4700, and 14,110 nM (0.015, 0.120, 0.390, 1.42, 4.7, and 14.11 uM) at the time of sampling, corresponding to approximately 5, 29, 56, 83, 94, and 98% RO, respectively, in rats. The ED50 for increaing in frequency of swimming and decreasing in immobility are ~0.3 and 0.7 mg/kg, respectively, corresponding to RO of ~30 and 50%. Rislenemdaz (1, 3, 10, and 30 mg/kg) significantly increases total distance traveling (P<0.01 for 1 mg/kg; P<0.001 for 3, 10, and 30 mg/kg) compare to vehicle control over the 60 min test.
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SynonymsMK-0657 | CERC-301 | MK 0657 | MK0657 | CERC 301 | CERC301
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PathwayMembrane Transporter/Ion Channel
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TargetiGluR
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RecptoriGluR
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Research AreaNeurological Disease
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IndicationDepression
Chemical Information
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CAS Number808732-98-1
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Formula Weight358.417
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Molecular FormulaC19H23FN4O2
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Purity>98% (HPLC)
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SolubilityDMSO : 150 mg/mL 418.52 mM
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SMILESCC1=CC=C(C=C1)COC(=O)N2CCC(C(C2)F)CNC3=NC=CC=N3
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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