GPCR19

GPCR19 agonists and antagonists act on a G protein-coupled receptor that is activated by bile acids. Takeda G protein-coupled receptor 5 (TGR5), also called G protein-coupled bile acid receptor 1 (GPBAR1), was described as a membrane bile acid receptor in 2002 and 2003. Bile acid binding raises cyclic adenosine monophosphate (cAMP) levels inside the cell. A 2009 mouse study showed that TGR5 signaling in enteroendocrine L cells promotes glucagon-like peptide-1 (GLP-1) release and controls glucose homeostasis. INT-777, BAR501 and TC-G 1005 are TGR5 agonists, while SBI-115 blocks the receptor. INT-767 and BAR502 also activate the farnesoid X receptor (FXR), a nuclear bile acid receptor.

3 Items

  • 5β-Cholestane-3α,7α,12α,25-tetrol
    Cat. No.
    A60412

    5β-Cholestane-3α,7α,12α,25-tetrol

    Synonyms: 3α,7α; 12α; 25-Tetrahydroxycoprostane

    5β-Cholestane-3α,7α,12α,25-tetrol is a potent TGR5 activator, exhibiting an EC50 of 1.36 μM. This bile acid alcohol plays a significant role in regulating metabolic processes and has shown promising biological activity relevant to energy expenditure and glucose metabolism. Additionally, it serves as a crucial disease marker in Cerebrotendinous xanthomatosis (CTX), making it valuable for research into bile acid signaling and related metabolic disorders.

    Out of stock

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  • Deoxycholic acid sodium hydrate
    Cat. No.
    A60414

    Deoxycholic acid sodium hydrate

    Synonyms: Cholanoic Acid sodium hydrate; Desoxycholic acid sodium hydrate

    Deoxycholic acid sodium hydrate is a bile acid that functions as an activator of the G protein-coupled bile acid receptor TGR5. It plays a significant role in lipid metabolism and has been implicated in various physiological processes, including glucose homeostasis and energy expenditure. This compound is commonly used in research applications focused on metabolic disorders, liver function, and signaling pathways influenced by bile acids.

    Out of stock

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  • 6ECA
    Cat. No.
    A60416

    6ECA

    6ECA is a selective activator of the TGR5 receptor, exhibiting an EC50 of 3.44 μM. This compound demonstrates no significant activity at the FXR, making it a useful tool for investigating the role of TGR5 in metabolic conditions. 6ECA is particularly applicable for research focused on diabesity and related disorders.

    Out of stock

    All 3 sizes

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