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
MK 0343 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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.
| 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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
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:
Keywords: MK 0343, supplier, MK0343, gabaa, subtype-selective, partial, agonists, α3, alpha3, a3, anxiolytics, brain, penetrant, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
