Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MRK-016 is a selective, orally bioavailable inverse GABAA α5 receptor agonist.
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (135.73 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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MRK-016 342652-67-9 Others MRK 016 MRK016 inhibitor inhibit