MRK-016

Catalog No.: A12046

GABAA α5 receptor agonist

MRK-016

MRK-016 Chemical Structure

CAS NO. 342652-67-9

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.

Availability: In stock

Package Price Qty
5 mg
$90.00
10 mg
$155.00
50 mg
$460.00
100 mg
$920.00
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Biological Activity

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.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 27.15 mL 135.73 mL 271.45 mL
0.5 mM 5.43 mL 27.15 mL 54.29 mL
1 mM 2.71 mL 13.57 mL 27.15 mL
5 mM 0.54 mL 2.71 mL 5.43 mL

*The above data is based on the productmolecular weight 368.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A12046
Actions Agonist
M. Wt 368.39
Formula C17H20N8O2
Solubility DMSO
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 342652-67-9
Synonyms MRK 016, MRK016
SMILES CN1N=CN=C1COC2=NN3C(C4=NOC(C)=C4)=NN=CC3=C2C(C)(C)C

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