Synonym
MK-0343; MK 0343; MK0343; MRK 409; MRK409; MRK-409.
IUPAC/Chemical Name
7-cyclobutyl-3-(2,6-difluorophenyl)-6-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine
InChi Key
GOIFCXRIFSYPFG-UHFFFAOYSA-N
InChi Code
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
SMILES Code
CN1N=CN=C1COC2=NN3C(C=C2C4CCC4)=NN=C3C5=C(F)C=CC=C5F
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist.
|
Solvent |
mg/mL |
mM |
comments |
Solubility |
DMSO |
144.9 |
364.55 |
|
Ethanol |
19.9 |
50.00 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
397.39
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 |
1.15 mL |
5.76 mL |
11.51 mL |
5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: 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. 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. 2011 Mar;25(3):314-28.
doi: 10.1177/0269881109354927. Epub 2010 Feb 10. PubMed PMID: 20147571.
2: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin
Pharmacol. 2008 Apr;30(3):231-51. PubMed PMID: 18597009.
3: 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.
Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABA(A) alpha2,3
subtype selective agonist, compared to lorazepam and placebo in healthy male
volunteers. J Psychopharmacol. 2008 Jan;22(1):24-32. doi:
10.1177/0269881107082108. PubMed PMID: 18187530.