产品信息
抗原名称
GPR109A
商品描述
MK-6892 is a highly potential GPR109A agonist with Ki value of 4.0 nM.
分子量
386.4018
纯度
>98%
外观
Powder
In vitro(体外研究)
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(体内研究)
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.
背景
别名
MK 6892;MK6892
分子式
C19H22N4O5
CAS号
917910-45-3
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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