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MRK-016

SKU: orb2893738

Description

MRK-016 is a selective GABAA α5 receptor inverse agonist/ negative allosteric modulator, (IC50=3 nM) with the advantages of being orally available and penetrating the blood-brain barrier.MRK-016 increases long time period potentiation (LTP) in mouse hippocampal slices, with memory-improvement, antidepressant, and pain-treating effects.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number342652-67-9
MW368.39
Purity99.76%
FormulaC17H20N8O2
SMILESN=1N=C(C2=NOC(=C2)C)N3N=C(OCC4=NC=NN4C)C(=C3C1)C(C)(C)C
TargetGABA Receptor
SolubilityDMSO:40 mg/mL (108.58 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.43 mM)

Bioactivity

Target IC50
GABAA α3β3γ2 (human):0.77 nM (Ki)|GABAA α5:3 nM (EC50)|GABAA α1β3γ2 (human):0.83 nM (Ki)|GABAA α2β3γ2 (human):0.85 nM (Ki)|GABAA α5β3γ2 (human):1.4 nM (Ki)
In Vivo
MRK-016 (0.3, 1 or 3 mg/kg, oral) exhibits cognitive enhancement activity in the delayed matching place version o the Morris water maze. MRK-016 (3 mg/kg, intraperitoneal) prevents LPS-induced learning/memory impairment in mice.
In Vitro
MRK-016 is a selective, orally bioavailable inverse MARKET α5 receptor agonist

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
DisclaimerFor research use only

Alternative Names

MRK 016, MRK016, MRK-016

Similar Products

  • MRK-016 [orb611735]

    >98%

    342652-67-9

    368.3931

    C17H20N8O2

    10 mg, 50 mg
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Key Properties

No computed properties available.

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Protocol Information

MRK-016 (orb2893738)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 90.00
5 mg
$ 140.00
1 ml x 10 mM (in DMSO)
$ 150.00
10 mg
$ 200.00
25 mg
$ 310.00
50 mg
$ 390.00
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