MK-6892 - GPR109A Agonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMK-6892Cat. No.: HY-10680CAS No.: 917910-45-3分式: CHNO分量: 386.4作靶点: GPR109A作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (129.40 mM; Need ultrasonic)Mass Solven

2、t1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5880 mL 12.9400 mL 25.8799 mL5 mM 0.5176 mL 2.5880 mL 5.1760 mL10 mM 0.2588 mL 1.2940 mL 2.5880 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您

3、配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.47 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.47 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.47 mM); Clear solution1/2 Mas

4、ter of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 MK-6892种有效的选择性烟酸 (NA) 受体 GPR109A 激动剂。MK-6892 作于 GPR109A 的 Ki 和 EC50分别为 4 nM 和 16 nM。IC50 & Target Ki: 4 nM (GPR109A) 1EC50: 16 nM (GPR109A) 1体外研究 MK-6892 evokes a potent internalization of GPR109A in U2OS -arrestin2-RrGFP cells.MK-6892

5、 shows anEC50 value of 74 nM on calcium mobilization assay 2.体内研究 MK-6892 is orally administered to WT or nicotinic acid (NA) receptor null mice on the same C57Bl/6 geneticbackground. After 15 min of 100 mg/kg dosing of MK-6892 to fed WT or NA receptor null mice, the bloodlevels of MK-6892 at 15 min

6、 are 229 M (950-fold greater than the in vitro EC50 determined in mouse NAreceptor GTPS assay, which is 240 nM) in WT mice and 148 M (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 receptornull animals, indicati

7、ng that the FFA reduction of MK-6892 is NA receptor-dependent. MK-6892 is selectedfor the studies because of its good PK and activity profiles in these two species (EC50=4.6 M in the GTPSassay for the rat NA receptor and 1.3 M in the GTPS assay for the dog NA receptor). Despite thesignificant weaker

8、 activity of MK-6892 in rat and dog with respect to that in human, MK-6892 shows goodactivity in reducing FFA in rat and dog models 1.户使本产品发表的科研献 Glia. 2018 Feb;66(2):256-278.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Shen HC, et al. Discovery of a biaryl cyclohexene carbo

9、xylic acid (MK-6892): a potent and selective high affinity niacin receptor fullagonist with reduced flushing profiles in animals as a preclinical candidate. J Med Chem. 2010 Mar 25;53(6):2666-70.2. Kim HY, et al. Discovery of 4-(phenyl)thio-1H-pyrazole derivatives as agonists of GPR109A, a high affinity niacin receptor. Arch PharmRes. 2015 Jun;38(6):1019-32.McePdfHeightCaution: Product has not been fully validated for me