1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR109A

GPR109A (G蛋白偶联受体109A)

GPR109A is a G-protein-coupled receptor for nicotinate but recognizes butyrate with low affinity. GPR109A is expressed in the lumen-facing apical membrane of colonic and intestinal epithelial cells and that the receptor recognizes butyrate as a ligand. The expression of GPR109A is silenced in colon cancer in humans, in a mouse model of intestinal/colon cancer, and in colon cancer cell lines. The tumor-associated silencing of GPR109A involves DNA methylation directly or indirectly. Reexpression of GPR109A in colon cancer cells induces apoptosis, but only in the presence of its ligands butyrate and nicotinate. Butyrate is an inhibitor of histone deacetylases, but apoptosis induced by activation of GPR109A with its ligands in colon cancer cells does not involve inhibition of histone deacetylation. The primary changes in this apoptotic process include down-regulation of Bcl-2, Bcl-xL, and cyclin D1 and up-regulation of death receptor pathway. In addition, GPR109A/butyrate suppresses nuclear factor-kappaB activation in normal and cancer colon cell lines as well as in normal mouse colon. These studies show that GPR109A mediates the tumor-suppressive effects of the bacterial fermentation product butyrate in colon.

GPR109A 相关产品 (6):

目录号 产品名 作用方式 纯度
  • HY-103252
    Monomethyl fumarate


    Agonist ≥98.0%
    Monomethyl fumarate 是 Dimethyl fumarate (DMF) 的活性代谢产物,一种有效的 GPR109A 激动剂。Monomethyl fumarate 具有用于多种神经保护途径和其他视网膜疾病模型的潜力。
  • HY-10680
    MK-6892 Agonist 99.43%
    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 KiEC50 分别为 4 nM 和 16 nM。
  • HY-13008
    MK-0354 Agonist 99.21%
    MK-0354是特异性的 GPR109a 受体激动剂, 作用于hGPR109a/mGPR109a, EC50分别为1.65 μM 和1.08 μM, 对GPR109b没有作用效果。
  • HY-119222
    GSK256073 Agonist ≥98.0%
    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。
  • HY-17585
    Mepenzolate bromide

    溴美喷酯; 溴化甲哌佐酯

    Inhibitor ≥98.0%
    Mepenzolate bromide 是一种有效的,具有口服活性的毒蕈碱受体拮抗剂,对 hM2RhM3RKi 分别为 0.68 和 2.6 nM。Mepenzolate bromide 可用于抑制与肠易激综合征相关的胃肠道过度运动。Mepenzolate bromide 是一种 GPR109A 抑制剂.
  • HY-107579
    Acifran Agonist
    Acifran (AY 25712) 是一种抗高血脂药物,是具有口服活性的 GPR109A (HM74A) 和 GPR109B(Niacin 的高亲和力和低亲和力受体)的激动剂。
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