GSK256073 is a potent, selective and orally activeGPR109Aagonist and a long-lasting and non-flushingHCA2full agonist with apEC₅₀of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia^[1][2]. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2

IC50: GPR109A (G-protein coupled receptor 109A); HCA2 (hydroxy-carboxylic acid receptor 2)^[1][2]

GSK256073 is approximately 10-fold more potent than niacin against human HCA2 (pEC₅₀value of 7.5 compared to 6.7 for niacin), has good activity versus the rat orthologue of HCA2 (pEC₅₀value of 6.9 compared to 6.4 for niacin) in membranes prepared from Chinese hamster ovary cellsexpressing recombinant human HCA2^[2].
GSK256073 (100 μM) suppresses cAMP elevation induced by isoprenaline (100 nM) in rat primary adipocytes^[2].

GSK256073 (oral adminstration; 1, 30 and 100 mg/kg; in rat) shows that the fall in NEFA is of rapid onset and that the maximum is dose-related with inhibitions of 74, 81 and 88%, respectively. Triglycerides decrease is followed as a similar pattern,although the duration was longer with a decrease of 91% still present 6 h post dose at 10 mg/kg^[2].
GSK256073 (intravenous injection; 1-10 mg/kg) produces a dose related decrease in NEFA. However, the increase in ear temperature induced by 10 mg/kg i.v. GSK256073 is only 40% of that induced by 10 mg/kg i.v. niacin^[2].

256.69

Solid

C₁₀H₁₃ClN₄O₂

862892-90-8

Room temperature in continental US; may vary elsewhere.

DMSO : 16.67 mg/mL(64.94 mM;Need ultrasonic)

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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 1.67 mg/mL (6.51 mM); Clear solution

  此方案可获得 ≥ 1.67 mg/mL (6.51 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。