MRK-016

MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.

Product Specifications

CAS Number

[342652-67-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/MRK-016.html

Purity

99.71

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CN1N=CN=C1COC2=NN3C(C4=NOC(C)=C4)=NN=CC3=C2C(C)(C)C

Molecular Formula

C17H20N8O2

Molecular Weight

368.39

Precautions

H302, H315, H319, H335

References & Citations

[1]Chambers MS, et al. An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. J Med Chem. 2004 Nov 18;47 (24) :5829-32.|[2]Atack JR, et al. In vitro and in vivo properties of 3-tert-butyl-7- (5-methylisoxazol-3-yl) -2- (1-methyl-1H-1,2,4-triazol-5-ylmethoxy) -pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist. J Pharmacol Exp Ther. 2009 Nov;331 (2) :470-84.|[3]Eimerbrink MJ, et al. Administration of the inverse benzodiazepine agonist MRK-016 rescues acquisition and memory consolidation following peripheral administration of bacterial endotoxin. Behav Brain Res. 2015 Jul 15;288:50-3.