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Rislenemdaz Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5753827

Rislenemdaz is an orally bioavailable and selective antagonist of N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B)(Ki and IC 50 of 8.1nM and 3.6nM, respectively). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Rislenemdaz, Inhibitor
Full Product Name
Rislenemdaz
Product Synonym Names
MK-0657; CERC-301
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
358.41
Solubility
DMSO: 100mg/mL (279.01mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C19H23FN4O2
SMILES
O=C(N1C[C@@H](F)[C@@H](CNC2=NC=CC=N2)CC1)OCC3=CC=C(C)C=C3
CAS Number
808732-98-1
Target & IC50
GluN2B: ic50 8.1nM (ki)
In Vitro
Rislenemdaz plasma levels are approximately 15, 120, 390, 1420, 4700, and 14,110nM (0.015, 0.120, 0.390, 1.42, 4.7, and 14.11uM) 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 0.7mg/kg, respectively, corresponding to RO of ~30 and 50%. Rislenemdaz (1, 3, 10, and 30mg/kg) significantly increases total distance traveling (P<0.01 for 1mg/kg; P<0.001 for 3, 10, and 30mg/kg) compare to vehicle control over the 60 min test.

Product References and Citations for Rislenemdaz, inhibitor

Rachel Garner, et al. Preclinical pharmacology and pharmacokinetics of CERC-301, a GluN2B-selective N-methyl-D-aspartate receptor antagonist. Pharmacol Res Perspect. 2015 Dec; 3(6): e00198.
Rachel Garner, et al. Preclinical pharmacology and pharmacokinetics of CERC-301, a GluN2B-selective N-methyl-D-aspartate receptor antagonist. Pharmacol Res Perspect. 2015 Dec; 3(6): e00198.

Other Notes

Small volumes of Rislenemdaz, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Rislenemdaz purchase

MBS5753827 is an inhibitor targeting Rislenemdaz.
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