[CAS NO. 917910-45-3] MK-6892
PRODUCTS SPECIFICATIONS [917910-45-3]
DESCRIPTION [917910-45-3]
Overview
| MDL | MFCD20528236 |
|---|---|
| Molecular Weight | 386.40 |
| Molecular Formula | C19H22N4O5 |
| SMILES | OC(C=C1)=CN=C1C2=NOC(CC(C)(C)C(NC3=C(C(O)=O)CCCC3)=O)=N2 |
1 Publications Citing Use of MCE
Summary
In Vitro
MK-6892 evokes a potent internalization of GPR109A in U2OS β-arrestin2-RrGFP cells.MK-6892 shows an EC 50 value of 74 nM on calcium mobilization assay [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MK-6892 is orally administered to WT or nicotinic acid (NA) receptor null mice on the same C57Bl/6 genetic background. After 15 min of 100 mg/kg dosing of MK-6892 to fed WT or NA receptor null mice, the blood levels of MK-6892 at 15 min are 229 μM (~950-fold greater than the in vitro EC 50 determined in mouse NA receptor GTPγS assay, which is 240 nM) in WT mice and 148 μM (~620-fold greater than the in vitro EC 50 ) in NA receptor null mice. MK-6892 effectively suppresses plasma FFA in the WT but not in the NA receptor null animals, indicating that the FFA reduction of MK-6892 is NA receptor-dependent. MK-6892 is selected for the studies because of its good PK and activity profiles in these two species (EC 50 =4.6 μM in the GTPγS assay for the rat NA receptor and 1.3 μM in the GTPγS assay for the dog NA receptor). Despite the significant weaker activity of MK-6892 in rat and dog with respect to that in human, MK-6892 shows good activity in reducing FFA in rat and dog models [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 : 50 mg/mL ( 129.40 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5880 mL | 12.9400 mL | 25.8799 mL |
| 5 mM | 0.5176 mL | 2.5880 mL | 5.1760 mL |
| 10 mM | 0.2588 mL | 1.2940 mL | 2.5880 mL |
References
- [1] Shen HC, et al. Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. J Med Chem. 2010 Mar 25;53(6):2666-70.
- [2] Kim HY, et al. Discovery of 4-(phenyl)thio-1H-pyrazole derivatives as agonists of GPR109A, a high affinity niacin receptor. Arch Pharm Res. 2015 Jun;38(6):1019-32.