MK-0343

• CAT Number: I008005
• CAS Number: 233275-76-8
• Molecular Formula: C19H17F2N7O
• Molecular Weight: 397.39
• Purity: ≥95%
• Target: GABA Receptor
• Solubility: Soluble in DMSO, not in water
• Storage: Store at +4C
• IUPAC Name: 7-cyclobutyl-3-(2,6-difluorophenyl)-6-[(2-methyl-1,2,4-triazol-3-yl)methoxy]-[1,2,4]triazolo[4,3-b]pyridazine
• InChI: InChI=1S/C19H17F2N7O/c1-27-16(22-10-23-27)9-29-19-12(11-4-2-5-11)8-15-24-25-18(28(15)26-19)17-13(20)6-3-7-14(17)21/h3,6-8,10-11H,2,4-5,9H2,1H3
• InChIKey: GOIFCXRIFSYPFG-UHFFFAOYSA-N
• SMILES: CN1C(=NC=N1)COC2=NN3C(=NN=C3C4=C(C=CC=C4F)F)C=C2C5CCC5

MK-0343 (CAT: I008005), also referred to as MRK-409, is a compound that acts as a selective partial agonist of the GABAA receptor subtype. It has been studied for its anxiolytic effects in preclinical models, showing promise as a potential treatment for anxiety disorders. Notably, in preclinical species, MK-0343 exhibits anxiolytic effects without causing sedation. However, it’s important to mention that in human studies, MK-0343 has been found to induce sedation, which has led to challenges in its clinical development as a non-sedating anxiolytic.

Reference

1:MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. Atack JR, Wafford KA, Street LJ, Dawson GR, Tye S, Van Laere K, Bormans G, Sanabria-Bohórquez SM, De Lepeleire I, de Hoon JN, Van Hecken A, Burns HD, McKernan RM, Murphy MG, Hargreaves RJ.J Psychopharmacol. 2011 Mar;25(3):314-28. doi: 10.1177/0269881109354927. Epub 2010 Feb 10. PMID: 20147571 2:Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABA(A) alpha2,3 subtype selective agonist, compared to lorazepam and placebo in healthy male volunteers. de Haas SL, de Visser SJ, van der Post JP, Schoemaker RC, van Dyck K, Murphy MG, de Smet M, Vessey LK, Ramakrishnan R, Xue L, Cohen AF, van Gerven JM.J Psychopharmacol. 2008 Jan;22(1):24-32. doi: 10.1177/0269881107082108. PMID: 18187530