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Tocris/MRK 016/3817/10/10 mg

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货号: 3817/10

品牌: Tocris

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Description: α5-selective GABA_A inverse agonist

Chemical Name: 3-(1,1-Dimethylethyl)-7-(5-methyl-3-isoxazolyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-pyrazolo[1,5-d][1,2,4]triazine

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

GABA_A receptor inverse agonist selective for the α5-subtype (EC₅₀ = 3 nM). Exhibits affinity at benzodiazepine binding site of recombinant human GABA_A receptors (K_i values are 0.77 nM, 0.83 nM, 0.85 nM and 1.4 nM for α3-, α1-, α2-, and α5-containing respectively). Increases long-term potentiation (LTP) in mouse hippocampal slices. Exhibits no anxiogenic or proconvulsant activity.

Licensing Information

Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)

Compound Libraries

MRK 016 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	368.39
Formula	C₁₇H₂₀N₈O₂
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	342652-67-9
PubChem ID	6918583
InChI Key	QYSYOGCIDRANAR-UHFFFAOYSA-N
Smiles	CC(C)(C)C2=C1C=NN=C(C4=NOC(C)=C4)N1N=C2OCC3=NC=NN3C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	36.84	100
	ethanol	3.68	10

Preparing Stock Solutions

The following data is based on the product molecular 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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.71 mL	13.57 mL	27.15 mL
5 mM	0.54 mL	2.71 mL	5.43 mL
10 mM	0.27 mL	1.36 mL	2.71 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Chambers et al (2004) An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABA_A α5 receptors with cognition enhancing properties. J.Med.Chem. 47 5829 PMID: 15537339

Atack et al (2009) 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 GABA_A receptor α5 subtype-selective inverse agonist. J.Pharmacol.Exp.Ther. 331 470 PMID: 19704033

Keywords: MRK 016, supplier, MRK016, GABA, a5, inverse, agonist, alpha5, GABAA, α5, merck, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience

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