MRK-016 is a selective, orally bioavailable inverse agonist of GABAA alpha5 receptor, with an EC50 of 3 nM for GABAA alpha5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA alpha1beta3gamma2, GABAA alpha2beta3gamma2, GABAA alpha3beta3gamma2, and GABAA alpha5beta3gamma2, respectively, MRK-016 also readily penetrates the CNS.
Molecular Weight:
368.39
Purity:
99.71
CAS Number:
[342652-67-9]
Formula:
C17H20N8O2
Target:
GABA Receptor
Application Notes:
Reference compound
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