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MRK-016

Catalog No. T12105   CAS 342652-67-9

MRK-016 is a selective, orally bioavailable inverse GABAA α5 receptor agonist.

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MRK-016 Chemical Structure
MRK-016, CAS 342652-67-9
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MRK-016 is a selective, orally bioavailable inverse GABAA α5 receptor agonist.
Targets&IC50 GABAA α5:3 nM (EC50), GABAA α1β3γ2 (human):0.83 nM (Ki), GABAA α3β3γ2 (human):0.77 nM (Ki), GABAA α2β3γ2 (human):0.85 nM (Ki), GABAA α5β3γ2 (human):1.4 nM (Ki)
In vitro MRK-016 is a selective, orally bioavailable inverse GABAA α5 receptor agonist(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)[1].
In vivo MRK-016 (0.3, 1, or 3 mg/kg p.o.) shows cognition-enhancing activity in the delayed matching-to-position version of the Morris water maze. MRK-016 (1, 3, or 10 mg/kg i.p.) does not produce kindling in mice[2]. MRK-016 (3 mg/kg, i.p.) protects against LPS-induced learning/memory decrements in mice[3].
Molecular Weight 368.39
Formula C17H20N8O2
CAS No. 342652-67-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (135.73 mM), sonification is recommended.

TargetMolReferences and Literature

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.

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Keywords

MRK-016 342652-67-9 Others MRK 016 MRK016 inhibitor inhibit

 

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