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Submit ReviewMK 0343
Description: GABAA partial agonist; displays subtype selectivity
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)
Biological Activity for MK 0343
MK 0343 is a 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.
Technical Data for MK 0343
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for MK 0343
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.74 | 100 | |
| ethanol | 19.87 | 50 |
Preparing Stock Solutions for MK 0343
The following data is based on the product molecular weight 397.38. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 2.52 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 for MK 0343
References for MK 0343
References are publications that support the biological activity of the product.
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 L.pam 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
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Keywords: MK 0343, MK 0343 supplier, MK0343, gabaa, subtype-selective, partial, agonists, α3, alpha3, a3, anxiolytics, brain, penetrant, GABAA, Receptors, 4415, Tocris Bioscience
Citations for MK 0343
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