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

GPR109A (G蛋白偶联受体109A)

HM74A; PUMA-G; HCA2; HCAR2 

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 (14):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-103252
    Monomethyl fumarate

    富马酸单甲酯

    Agonist 98.50%
    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。
    Monomethyl fumarate
  • HY-17585
    Mepenzolate bromide

    溴美喷酯

    Inhibitor 99.90%
    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.
    Mepenzolate bromide
  • HY-135982
    GPR81 agonist 1 99.78%
    GPR81 agonist 1 是一种高效、高选择性的 GPR81 激动剂,对人和小鼠 GPR81 的EC50 分别为 58 nM 和 50 nM。GPR81 agonist 1 抑制分化的 3T3-L1 脂肪细胞的脂解。GPR81 agonist 1 抑制小鼠的脂解并不会造成皮肤潮红。GPR81 agonist 1 对 GPR81 的选择性高于 GPR109a
    GPR81 agonist 1
  • 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 GPR109AKiEC50 分别为 4 nM 和 16 nM。
    MK-6892
  • HY-13008
    MK-0354 Agonist 99.73%
    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。
    MK-0354
  • HY-119222
    GSK256073 Agonist 99.11%
    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。
    GSK256073
  • HY-107581
    MK-1903 99.92%
    MK-1903 是一种有效且选择性的羟基羧酸受体2 (HCA2, GPR109A) 的完全激动剂。
    MK-1903
  • HY-107579
    Acifran Agonist 99.25%
    Acifran (AY 25712) 是一种抗高血脂活性分子,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。
    Acifran
  • HY-W095200
    GPR109 receptor agonist-2 Agonist 99.08%
    GPR109 receptor agonist-2 (Compound 5) 是一种选择性的 GPR109a 激动剂,其 pEC50 为 5.53。
    GPR109 receptor agonist-2
  • HY-107580
    GPR109 receptor agonist-1 Agonist 99.91%
    GPR109 receptor agonist-1 (Compound 3a) 是一种高选择性的人孤儿 G 蛋白偶联受体 GPR109b 激动剂,pEC50 为 6.4。GPR109 receptor agonist-1 可用于心脏代谢疾病的研究。
    GPR109 receptor agonist-1
  • HY-47823
    GPCR agonist-2 99.93%
    GPCR agonist-2 (Compound 5j) 是一种 GPCR GPR109b (HM74) 激动剂,pEC50 值为 6.51。GPCR agonist-2 可用于脂质紊乱相关疾病的研究。
    GPCR agonist-2
  • HY-103252S1
    Monomethyl fumarate-d5

    富马酸单甲酯-d5

    Agonist
    Monomethyl fumarate-d5 是 Monomethyl fumarate 氘代物。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。
    Monomethyl fumarate-d<sub>5</sub>
  • HY-103252S
    Monomethyl fumarate-d3

    富马酸单甲酯 d3

    98.57%
    Monomethyl fumarate-d3 是 Monomethyl fumarate 的氘代化合物。Monomethyl fumarate 是富马酸二甲酯的主要代谢物。
    Monomethyl fumarate-d<sub>3</sub>
  • HY-148563
    GPR81 agonist 2
    GPR81 agonist 2 (compound 1) 是一种有效的 GPR81 激动剂,对于 hGPR81、hGPR109A 的 EC50 值分别为 0.023、0.123 µM。
    GPR81 agonist 2