MedKoo Cat#: 526627 | Name: MK-0343
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MK-0343, also known as MRK-409, is a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. MRK-409 binds to α1-, α2-, α3- and α5-containing human recombinant GABA(A) receptors with comparable high affinity (0.21-0.40 nM). However, MRK-409 has greater agonist efficacy at the α3 compared with α1 subtypes (respective efficacies relative to the full agonist chlordiazepoxide of 0.45 and 0.18).

Chemical Structure

MK-0343
MK-0343
CAS#233275-76-8

Theoretical Analysis

MedKoo Cat#: 526627

Name: MK-0343

CAS#: 233275-76-8

Chemical Formula: C19H17F2N7O

Exact Mass: 397.1463

Molecular Weight: 397.39

Elemental Analysis: C, 57.43; H, 4.31; F, 9.56; N, 24.67; O, 4.03

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 weeks
10mg USD 650.00 2 weeks
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Related CAS #
No Data
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
Appearance
Solid powder
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
More Info
Product Data
Biological target:
MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist.
In vitro activity:
TBD
In vivo activity:
TBD
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.

Recalculate based on batch purity %
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
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
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.