MK 0343

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Cat.No. 4415 - MK 0343 | C19H17F2N7O | CAS No. 233275-76-8
Description: Subtype-selective GABAA receptor partial agonist
Chemical Name: 7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazo[4,3-b]pyridazine
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Subtype-selective GABAA partial agonist (Ki values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively); occupies the benzodiazepine site of GABAA receptors. Displays greater agonist efficacy at α3 compared to α1. Exhibits anxiolytic and non-sedating properties in rodent models. Brain penetrant.

Compound Libraries

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Technical Data

M. Wt 397.38
Formula C19H17F2N7O
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 233275-76-8
PubChem ID 22609888
InChI Key GOIFCXRIFSYPFG-UHFFFAOYSA-N
Smiles FC(C=CC=C3F)=C3C1=NN=C2N1N=C(OCC5=NC=NN5C)C(C4CCC4)=C2

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 39.74 100
ethanol 19.87 50

Preparing Stock Solutions

The following data is based on the product molecular weight 397.38. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.52 mL 12.58 mL 25.16 mL
5 mM 0.5 mL 2.52 mL 5.03 mL
10 mM 0.25 mL 1.26 mL 2.52 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Atack et al (2011) MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. J.Psychopharmacol. 25 314 PMID: 20147571

de Haas et al (2008) Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABAA α2,3 subtype-selective agonist, compared to lorazepam and placebo in healthy male volunteers. J.Psychopharmacol. 22 24 PMID: 18187530

Atack et al (2010) Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, prima J.Pharmacol.Exp.Ther. 332 17 PMID:


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Keywords: MK 0343, supplier, MK0343, gabaa, subtype-selective, partial, agonists, α3, alpha3, a3, anxiolytics, brain, penetrant, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience

Citations for MK 0343

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