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MK-6892

CAS No. : 917910-45-3

MCE 站：MK-6892

产品活性：MK-6892 是一种有效的选择性烟酸 (NA) 受体 GPR109A 激动剂。MK-6892 作用于人 GPR109A 的 K_i 和 EC₅₀ 分别为 4 nM 和 16 nM。

研究领域：GPCR/G Protein

作用靶点：GPR109A

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.

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. MK-6892 is selected for the studies because of its good PK and activity profiles in these two species (EC₅₀=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.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Anti-Cancer Compound Library  |  Monomethyl fumarate

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