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GSK256073

CAS No. : 862892-90-8

MCE 站：GSK256073

产品活性：GSK256073 是一种有效的、选择性的、口服活性的 GPR109A 激动剂，是一种持久的 HCA2 激动剂，其 pEC₅₀ 为 7.5 (Human HCA2)。GSK256073 可通过抑制脂降解而明显改善葡萄糖稳态，具有研究 2 型糖尿病 (T2DM) 和血脂异常的潜力。

研究领域：GPCR/G Protein

作用靶点：GPR109A

In Vitro: GSK256073 is approximately 10-fold more potent than niacin against human HCA2 (pEC₅₀ value of 7.5 compared to 6.7 for niacin), has good activity versus the rat orthologue of HCA2 (pEC₅₀ value of 6.9 compared to 6.4 for niacin) in membranes prepared from Chinese hamster ovary cellsexpressing recombinant human HCA2.
GSK256073 (100 μM) suppresses cAMP elevation induced by isoprenaline (100 nM) in rat primary adipocytes.

In Vivo: 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.
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.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Diabetes Related Compound Library  |  Monomethyl fumarate

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