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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 | Price | Availability | Quantity |
---|---|---|---|
1 mg | $98 | In Stock | |
5 mg | $198 | In Stock | |
10 mg | $297 | In Stock | |
25 mg | $497 | In Stock | |
50 mg | $689 | In Stock | |
100 mg | $993 | In Stock | |
500 mg | $1,980 | In Stock | |
1 mL x 10 mM (in DMSO) | $243 | In Stock |
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 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 administered orally to WT and nicotinic acid (NA) receptor null mice on a C57Bl/6 genetic background. Following a 100 mg/kg dose, blood levels of MK-6892 reach 229 μM in WT mice and 148 μM in NA receptor null mice after 15 minutes, significantly exceeding the in vitro EC50 (240 nM). MK-6892 effectively suppresses plasma FFA in WT mice, but not in NA receptor null mice, indicating NA receptor-dependent FFA reduction [1]. |
Molecular Weight | 386.4 |
Formula | C19H22N4O5 |
Cas No. | 917910-45-3 |
Smiles | CC(C)(Cc1nc(no1)-c1ccc(O)cn1)C(=O)NC1=C(CCCC1)C(O)=O |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (116.46 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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