1. Signaling Pathways
  2. GPCR/G Protein
  3. G protein-coupled Bile Acid Receptor 1

G protein-coupled Bile Acid Receptor 1 (胆汁酸受体)

G-protein coupled receptor 19; GPCR19; TGR5; GPBAR1

G protein-coupled bile acid receptor 1 (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.

G protein-coupled Bile Acid Receptor 1 相关产品 (44):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101273
    BAR502 Agonist 99.53%
    BAR502是FXRGPBAR1的双重激动剂,IC50值分别为2 μM 和0.4 μM。
    BAR502
  • HY-N0593S3
    Deoxycholic acid-13C

    去氧胆酸-13C

    Activator 98.00%
    Deoxycholic acid-13C 是一种 13C 标记的 Deoxycholic acid。Deoxycholic acid 激活 G 蛋白偶联胆汁酸受体TGR5
    Deoxycholic acid-<sup>13</sup>C
  • 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。
    PEN (rat)
  • HY-126855
    Cholic acid 7-sulfate Agonist 99.90%
    Cholic acid 7-sulfate (7-Sulfocholic acid),一种 Cholic acid 的代谢物,是 TGR5 激动剂。Cholic acid 7-sulfate 可增加 Tgr5 表达并诱导 GLP-1 分泌。
    Cholic acid 7-sulfate
  • HY-145234
    GPBAR1-IN-3 Agonist
    GPBAR1-IN-3 (Compound 14) 是一种选择性 GPBAR1 激动剂 (EC50=0.17 μM) 和 CysLT1R 拮抗剂。
    GPBAR1-IN-3
  • HY-13771S
    Ursodeoxycholic acid-d5

    熊去氧胆酸 d5

    Agonist
    Ursodeoxycholic acid-d5 是 Ursodeoxycholic acid 的氘代物。Ursodeoxycholic acid (Ursodeoxycholate) 是由肠道细菌转化 (cheno)脱氧胆酸而产生的一种次级胆汁酸,是肠道屏障完整性的关键调节因子,对脂质代谢至关重要。Ursodeoxycholic acid 作为信号分子,通过与胆汁酸激活的受体相互作用发挥作用,包括G蛋白偶联的胆汁酸受体5 (TGR5GPCR19) 和法尼酯X受体 (FXR)。Ursodeoxycholic acid 可用于多种肝脏和胃肠道疾病的研究。具有口服活性。
    Ursodeoxycholic acid-d<sub>5</sub>
  • HY-149807
    TGR5 agonist 1 Agonist
    TGR5 agonist 1 (compound 18) 是一种有效的 TGR5 激动剂,EC50 值为 0.31 µM。
    TGR5 agonist 1
  • HY-N0593S2
    Deoxycholic acid-d6

    去氧胆酸 d6

    Activator
    Deoxycholic acid-d6 是 Deoxycholic acid 的氘代物。Deoxycholic acid 激活 G 蛋白偶联胆汁酸受体TGR5
    Deoxycholic acid-d<sub>6</sub>
  • HY-155307
    TGR5 agonist 4 Agonist
    TGR5 agonist 4(化合物 19)是一种胆酸衍生物,是一种选择性 TGR5 激动剂,EC50 为 4 μM。
    TGR5 agonist 4
  • HY-147086
    CAY10789 Agonist 99.84%
    CAY10789 (化合物 6) 是一种有效的 CysLT1R 拮抗剂 (IC50=2.80 μM) 和 GPBAR1 激动剂 (EC50=3 μM)。CAY10789 显著降低 U937 细胞对 HAEC 的粘附,降低 TNF-α 的表达。CAY10789 具有良好的代谢稳定性和良好的药代动力学。 CAY10789 可用于结肠炎、代谢综合征等 GPBAR1/CysLT1R 相关疾病的研究。
    CAY10789
  • HY-107612
    GPBAR-A Agonist
    GPBAR-A 是一种特异性的胆汁酸受体 GPBAR1 的激动剂。GPBAR-A 可用于糖尿病的研究。
    GPBAR-A
  • HY-155306
    TGR5 agonist 3 Agonist
    TGR5 agonist 3(化合物 8)是一种胆酸衍生物,是一种选择性 TGR5 激动剂,EC50 为 5 μM。
    TGR5 agonist 3
  • HY-133862
    SCH-202676 Modulator
    SCH-202676 是一种 G 蛋白偶联受体 (GPCRs) 和腺苷受体 (adenosine receptor (AR)) 调节剂。SCH-202676 具有抗流感活性,以时间依赖的方式抑制 3CLproIC50 为 0.655 µM。
    SCH-202676
  • HY-139677A
    5-HT7R antagonist 1 free base Antagonist
    5-HT7R antagonist 1 (free base) 是一种针对 5-HT7RKi = 6.5 nM)的G蛋白偏向性拮抗剂。
    5-HT7R antagonist 1 free base
  • HY-B0575R
    Triamterene (Standard)

    氨苯蝶啶(标准品)

    Inhibitor 99.92%
    Triamterene (Standard) 是 Triamterene 的分析标准品。本产品用于研究及分析应用。Triamterene是压敏型上皮钠离子通道(ENaC)阻断剂,有利尿作用。
    Triamterene (Standard)
  • HY-142159
    FXR/TGR5 agonist 1 Agonist
    FXR/TGR5 agonist 1 对 FXRTGR5 具有激动作用,可用于研究脂肪肝。
    FXR/TGR5 agonist 1
  • HY-139677
    5-HT7R antagonist 1 Antagonist
    5-HT7R antagonist 1 是一种针对 5-HT7RKi = 6.5 nM)的G蛋白偏向性拮抗剂。
    5-HT7R antagonist 1
  • HY-N0169S
    Hyodeoxycholic acid-d5

    猪去氧胆酸 d5

    Agonist
    Hyodeoxycholic acid-d5 是 Hyodeoxycholic acid 的氘代物。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。
    Hyodeoxycholic acid-d<sub>5</sub>
  • HY-149808
    TGR5 agonist 2 Agonist
    TGR5 agonist 2 (compound 19) 是一种有效的 TGR5 激动剂,EC50 值为 0.27 µM。
    TGR5 agonist 2
  • HY-146453
    TGR5 Receptor Agonist 3 Agonist
    TGR5 Receptor Agonist 3 (Compound 19) 是 G 蛋白偶联胆汁酸受体 1(GPBAR1,TGR5)激动剂软药化合物,具有降低胆囊充盈效果(良好的胆囊安全性),对 hTGR5 和 mTGR5 的 EC50 分别为 16.4 和 209 nM。
    TGR5 Receptor Agonist 3