G protein-coupled Bile Acid Receptor 1 Activator

ZY12201 is a selective and orally active TGR5 agonist and pan-CYP inhibitor. ZY12201 lowers glucose levels. ZY12201 induces enzymes regulated through Aryl Hydrocarbon Receptor, Constitutive Androstane Receptor, and Pregnane X Receptor. ZY12201 can be used for the research of type 2 diabetes.

Glycocholic acid-¹³C₂,d₄ is the deuterium labeled and ¹³C-labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

Hyocholic Acid (Standard) is the analytical standard of Hyocholic Acid. This product is intended for research and analytical applications. Hyocholic Acid is a bile acid found in pig. Hyocholic Acid can also be found in urine samples from patients with cholestasis. Hyocholic Acid promotes GLP-1 secretion via activating TGR5 and inhibiting FXR in enteroendocrine cells. Hyocholic Acid is known for its exceptional resistance to type 2 diabetes [1][2][3].

Hyocholic Acid-d₅ is the deuterium labeled Hyocholic Acid.

FXR agonist 17 is an orally active, steroidal FXR agonist with EC₅₀ values of 42.2 nM (TR-FRET) and 176.4 nM (luciferase reporter assay), respectively. FXR agonist 17 activates TGR5 (EC₅₀ = 2.6 μM) but does not activate hMRGPRX4. FXR agonist 17 exerts anti-inflammatory, hepatoprotective and antifibrotic effects, improves the non-alcoholic steatohepatitis (NAFLD) activity score and reduces the severity of liver fibrosis. FXR agonist 17 can be used for the research of NAFLD, cholestatic liver disease and liver fibrosis.

5β-Cholestane-3α,7α,12α,25-tetrol (3α,7α,12α,25-Tetrahydroxycoprostane) is a bile acid alcohol. 5β-Cholestane-3α,7α,12α,25-tetrol is a GPBAR1 (also known as TGR5) activator (EC₅₀: 1.36 μM). 5β-Cholestane-3α,7α,12α,25-tetrol is the predominant bile-alcohol disease marker present in patients with Cerebrotendinous xanthomatosis (CTX).

(Rac)-Pinostrobin ((±)-Pinostrobin) is a dual agonist of TGR5 and PPARγ. (Rac)-Pinostrobin specifically activates TGR5 without acting on other endogenously expressed GPCRs. (Rac)-Pinostrobin exhibits moderate PPARγ activation activity. (Rac)-Pinostrobin possesses metabolic regulatory activity. (Rac)-Pinostrobin can be used in research related to obesity and type 2 diabetes.

Deoxycholic acid (cholanoic acid) sodium hydrate, a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5.

Glycocholic acid (sodium) (Standard) is the analytical standard of Glycocholic acid sodium (HY-N1423A). This product is intended for research and analytical applications. Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

(E)-Methyl 4-coumarate (Standard) is the analytical standard of (E)-Methyl 4-coumarate. This product is intended for research and analytical applications. (E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as Allium cepa or Morinda citrifolia L. leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.

6ECA is a selective TGR5 receptor activator with an EC₅₀ of 3.44 μM. 6ECA shows no significant activity at FXR. 6ECA can be used for the study of diabesity.