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MRK-016

MRK-016

Item no.	HY-100370-25mg
Manufacturer	MedChem Express
CASRN	342652-67-9
Amount	25 mg
Quantity options	10 mM/1 mL 10 mg 1 mg 25 mg 50 mg 5 mg
Category	Neuroscience Neural Lineage Markers Metabolism Diabetes Glucose Homeostasis Inhibitors & Compound Libraries Small Molecules Neuronal Cell Markers
Type	Inhibitors
Specific against	other
Purity	99.71
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.
Smiles	CN1N=CN=C1COC2=NN3C(C4=NOC(C)=C4)=NN=CC3=C2C(C)(C)C
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Cancer-programmed cell death
Manufacturer - Targets	GABA Receptor
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	368.39
Product 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.
Manufacturer - Research Area	Cancer
Solubility	DMSO: 50 mg/mL (ultrasonic)
Manufacturer - Pathway	Membrane Transporter/Ion Channel; Neuronal Signaling
Clinical information	No Development Reported

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HY-100370-25mg-safety-datasheet.pdf