Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 115.00 | |
5 mg | In stock | $ 247.00 | |
10 mg | In stock | $ 356.00 | |
25 mg | In stock | $ 596.00 | |
50 mg | In stock | $ 839.00 | |
100 mg | In stock | $ 1,160.00 | |
500 mg | In stock | $ 2,320.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 260.00 |
Description | MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM). |
Targets&IC50 | GPR109A:16 nM (EC50), GPR109A:4 nM (Ki) |
In vitro | MK-6892 evokes a potent internalization of GPR109A in U2OS β-arrestin2-RrGFP cells.MK-6892 shows an EC50 value of 74 nM on calcium mobilization assay [2]. |
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 EC50 determined in mouse NA receptor GTPγS assay, which is 240 nM) in WT mice and 148 μM (~620-fold greater than the in vitro EC50) 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 [1]. |
Molecular Weight | 386.4 |
Formula | C19H22N4O5 |
CAS No. | 917910-45-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (129.40 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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MK-6892 917910-45-3 Endocrinology/Hormones GPCR/G Protein GPR HCAR2 PUMA-G HM74A HCA2 Inhibitor MK 6892 GPR109A inhibit MK6892 inhibitor