[CAS NO. 233275-76-8] MK-0343
PRODUCTS SPECIFICATIONS [233275-76-8]
DESCRIPTION [233275-76-8]
Overview
| MDL | MFCD22683821 |
|---|---|
| Molecular Weight | 397.38 |
| Molecular Formula | C19H17F2N7O |
| SMILES | CN1N=CN=C1COC2=NN3C(C=C2C4CCC4)=NN=C3C5=C(F)C=CC=C5F |
Summary
MK0343 (MRK-409) is an orally bioavailable GABA A receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic [1] .
IC50 & Target
Ki: 0.22 nM (rGABA A α1), 0.4 nM (rGABA A α2) , 0.21 nM (rGABA A α3), 78 nM (rGABA A α4), 0.23 nM (rGABA A α5), 980 nM (rGABA A α6) [1]
In Vivo
MK0343 readily penetrates the brain in rats and occupies the benzodiazepine site of GABAA receptors, measured using an in vivo [
3
H]flumazenil binding assay, with an Occ
50
of 2.2 mg/kg p.o. and a corresponding plasma EC
50
of 115 ng/mL
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague-Dawley rats (approximately 250–300g) (pharmacokinetics) [1] |
| Dosage: | 1, 2 or 3 mg/kg |
| Administration: | Oral administration |
| Result: | Readily penetrated the brain in rats and occupies the benzodiazepine site of GABAA receptors, with an Occ 50 of 2.2 mg/kg p.o. and a corresponding plasma EC 50 of 115 ng/mL. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 629.12 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5165 mL | 12.5824 mL | 25.1648 mL |
| 5 mM | 0.5033 mL | 2.5165 mL | 5.0330 mL |
| 10 mM | 0.2516 mL | 1.2582 mL | 2.5165 mL |
