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MRK-016

CAT: 0804-HY-100370-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-100370-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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.
CAS Number
342652-67-9
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
GABA Receptor
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Neuronal Signaling
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/MRK-016.html
Purity
99.71
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
CN1N=CN=C1COC2=NN3C(C4=NOC(C)=C4)=NN=CC3=C2C(C)(C)C
Molecular Formula
C17H20N8O2
Molecular Weight
368.39
Precautions
H302, H315, H319, H335
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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