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).
説明 | MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM). |
ターゲット&IC50 | GPR109A:16 nM (EC50), GPR109A:4 nM (Ki) |
In vitro | MK-6892 effectively induces the internalization of GPR109A in U2OS β-arrestin2-RrGFP cells and demonstrates a potent EC50 of 74 nM in calcium mobilization assays [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]. |
分子量 | 386.4 |
分子式 | 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), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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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