1. Signaling Pathways
  2. GPCR/G Protein
  3. GPCR19

GPCR19 (G蛋白偶联受体19)

GPCR19 (TGR5, GPBAR1) is a plasma membrane-bound, G protein-coupled receptor that has bile acids as its ligand. GPCR19 is a regulator of energy homeostasis, bile acid homeostasis as well as glucose metabolism. GPCR19 transduces extracellular signals through heterotrimeric G proteins.

GPCR19 can be activated by bile acids and then it induces cAMP production. As a membrane receptor, GPCR19 can be internalized into the cytoplasm in response to its ligands. GPCR19 plays important roles in cell signaling pathways such as nuclear factor κB (NF-κB), AKT, and extracellular signal-regulated kinases (ERK). Its agonists may be potential drugs for the treatment of metabolic, inflammation, and digestive disorders. In addition, GPCR19 stimulates glucagon-like peptide 1 (GLP-1) secretion. It also has become an attractive therapeutic target for the prevention and/or the treatment of obesity and its highly associated Type II diabetes and metabolic syndrome.

GPCR19 相关产品 (15):

目录号 产品名 作用方式 纯度
  • HY-15677
    INT-777 Agonist ≥98.0%
    INT-777是有效的 TGR5 激动剂,EC50 为 0.82 μM。
  • HY-N0593
    Deoxycholic acid Activator ≥98.0%
    Deoxycholic acid 激活 G 蛋白偶联胆汁酸受体TGR5
  • HY-111534
    SBI-115 Antagonist 99.57%
    SBI-115 是一种 TGR5 (GPCR19) 拮抗剂。SBI-115 通过抑制 TGR5 降低多囊性肝病的肝囊肿形成。
  • HY-14229
    TGR5 Receptor Agonist Agonist 99.85%
    TGR5 Receptor Agonist (CCDC) 是 TGR5(GPCR19) 激动剂。
  • HY-B0575
    Triamterene Inhibitor 99.98%
    Triamterene是压敏型上皮钠离子通道(ENaC)阻断剂,有利尿作用。
  • HY-N0593A
    Deoxycholic acid sodium salt Activator ≥98.0%
    Deoxycholic acid sodium salt 激活 G 蛋白偶联胆汁酸受体TGR5
  • HY-N0169
    Hyodeoxycholic acid Agonist ≥99.0%
    Hyodeoxycholic acid 是有肠道菌群在小肠中形成的次级胆汁酸,为 TGR5 (GPCR19) 的激动剂,在 CHO 细胞中,EC50 值为 31.6 µM。
  • HY-12434
    INT-767 Agonist ≥98.0%
    INT-767 是法尼醇 X 受体 (FXR)/TGR5双激动剂,EC50 值分别为 30 和 630 nM。
  • HY-101274
    BAR501 Agonist ≥98.0%
    BAR501是高效选择性的GPBAR1激动剂,EC50值为1 μM。
  • HY-102016
    SB756050 Agonist 99.32%
    SB756050 是选择性的 TGR5 激动剂。SB756050有潜力用于二型糖尿病的研究。
  • HY-101273
    BAR502 Agonist ≥98.0%
    BAR502是FXRGPBAR1的双重激动剂,IC50值分别为2 μM 和0.4 μM。
  • HY-15677A
    INT-777 R-enantiomer Agonist
    INT-777 R-enantiomer 是 INT-77 的 R 型异构体,对 TGR5 的 EC50 值为 4.79 μM,活性比 INT-777 低。
  • HY-110173
    TC-G 1005 Agonist 99.91%
    TC-G 1005 是一种有效,选择性和口服活性的 TGR5 激动剂,激活 hTGR5 和 mTGR5 的 EC50 值分别为 0.72 和 6.2 nM。TC-G 1005 可降低小鼠体内葡萄糖水平。
  • HY-P2278
    PEN (human) Agonist
    PEN (human) 是由 ProSAAS 原蛋白衍生而来的最丰富的下丘脑神经肽之一,是 GPR83 的内源性配体。
  • HY-P2277
    PEN (rat) Agonist
    PEN (rat) 是由 ProSAAS 原蛋白衍生而来的最丰富的下丘脑神经肽之一,是 GPR83 的内源性配体。
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