1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR120

GPR120 (G蛋白偶联受体120)

GPR120 (Free fatty acid receptor 4, FFA4) is a G protein-coupled receptor that acts as a sensor of long-chain fatty acids, modulates metabolism, and whose dysfunction participates in endocrine disturbances. In humans, two isoforms, long and short, of GPR120 receptors have been reported. Human GPR120 receptors couples with Gαq/11 and activates phospholipase C, leading to the hydrolysis of phosphatidylinositol 4, 5-bisphosphate, generating inositol trisphosphate and diacylglycerol. Inositol trisphosphate triggers calcium release from intracellular stores, whereas diacylglycerol, together with calcium, activates protein kinase C.

GPR120 has been shown to be densely expressed in human lungs and colon, as well as in adipocytes and macrophages, where it recognizes long-chained FFAs including palmitic acid, oleic acid, myristic acid, and importantly, the family of polyunsaturated omega-3 fatty acids, including α-linolenic acid (ALA), eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA). Agonism of GPR120 has been shown to mediate endocrine processes including secretion of glucagon-like peptide-1 (GLP-1) and cholecystokinin from intestinal enteroendocrine cells, inhibition of ghrelin secretion from gastric ghrelin cells, and regulation of adipocyte differentiation. GPR120 agonism has been shown to modulate numerous anti-inflammatory and insulin-sensitizing effects including suppression of TNF-α and IL-6 secretion from macrophages and enhancement of GLUT4 translocation and glucose uptake in adipocytes. GPR120 is a potential novel therapeutic target for the treatment of type 2 diabetes mellitus (T2DM).

GPR120 相关产品 (11):

目录号 产品名 作用方式 纯度
  • HY-100881
    TUG-891 Agonist 99.20%
    TUG-891 是有效的,选择性的长链游离脂肪酸受体 4 (FFA4/GPR120) 的激动剂。
  • HY-19995
    GSK137647A Agonist 99.51%
  • HY-19996
    AH-7614 Antagonist ≥99.0%
    AH-7614 是一种有效和选择性的 FFA4 (GPR120) 拮抗剂,对人,小鼠和大鼠 FFA4 的 pIC50 值分别为 7.1,8.1 和 8.1。AH-7614 对 FFA4 的选择性高于 FFA1 (pIC50<4.6)。AH-7614 能够阻断多不饱和 ω-6 脂肪酸亚油酸和 FFA4 激动剂的作用。
  • HY-101492
    GPR120 Agonist 3 Agonist 99.08%
    GPR120 Agonist 3 是选择性的Gpr120激动剂,logEC50值为 −7.62。
  • HY-N0040
    Ginsenoside Rb2 Activator ≥98.0%
    Ginsenoside Rb2 是人参提取物的主要生物活性成分之一。Ginsenoside Rb2 可以上调 GPR120 基因表达。Ginsenoside Rb2 具有抗病毒作用。
  • HY-111353
    GPR120 Agonist 2 Agonist 99.07%
    GPR120 Agonist 2 是一个 GPR120 激动剂,来自专利 US 20110313003 A1,实例 209。
  • HY-N3977
    Grifolic acid Agonist ≥98.0%
    Grifolic acid 是一种酚类化合物,从 Albatrellus confluens 蘑菇中提取。Grifolic acid 作为游离脂肪酸受体 (FFAR4/GPR120) 的激动剂。
  • HY-50162
    GPR120 modulator 1 Modulator 98.62%
    GPR120 modulator 1 是 G 蛋白偶联受体 120 (GPR120) 的调制器。详细信息请参考专利文献 US8394841B2 中 的化合物 F1。GPR120 modulator 1 可用于 GPR120 异常或失调相关疾病的研究,如糖尿病。
  • HY-50172
    GPR120 modulator 2 Modulator
    GPR120 modulator 2 是 G 蛋白偶联受体 120 (GPR120) 的调制器。详细信息请参考专利文献 US8394841B2 中 的化合物 F13。GPR120 modulator 2 可用于 GPR120 异常或失调相关疾病的研究,如糖尿病。
  • HY-108711
    GPR120 Agonist 1 Agonist
    GPR120 Agonist 1 是一种有效、选择性的 GPR120 激动剂,具有良好的抗糖尿病作用和安全性,可作为开发候选药物。
  • HY-P1123
    MEDICA16 Agonist
    MEDICA16 是一种 ATP-citrate lyase 抑制剂,能显著降低腓肠肌细胞内 TG 的含量,这种降低伴随着胰岛素敏感性的增加。MEDICA16 是 GPR40 的选择性激动剂,也是 GPR120 的选择性部分激动剂。
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