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human TGR5

" in MedChemExpress (MCE) Product Catalog:

By Targets:	G protein-coupled Bile Acid Receptor 1 (6) Cytochrome P450 (1) FXR (1) Heme Oxygenase (HO) (1) Keap1-Nrf2 (1) Quinone Reductase (1) Somatostatin Receptor (1) TNF Receptor (1)
By Research Areas:	Cardiovascular Disease (1) Inflammation/Immunology (2) Metabolic Disease (5)

Inhibitors & Agonists

Recombinant Proteins

Targets Recommended: G protein-coupled Bile Acid Receptor 1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-120565

WB403	G protein-coupled Bile Acid Receptor 1	Metabolic Disease
WB403 is an orally active *TGR5* activator with an EC₅₀ of 5.5 μM against human *TGR5. WB403 activates TGR5* to stimulate downstream signaling pathways, promote GLP-1 secretion, improve glucose tolerance in mice with type 2 diabetes, and reduce levels of fasting blood glucose, postprandial blood glucose and HbA1c. WB403 increases pancreatic β-cell mass and restores the distribution of α-cells and β-cells in islets. WB403 is applicable to the research of type 2 diabetes .

HY-182905

SSTR5/TGR5-modulator-1	Somatostatin Receptor G protein-coupled Bile Acid Receptor 1	Metabolic Disease
SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human *TGR5* and human SSTR5. SSTR5/TGR5-modulator-1 activates human *TGR5* to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus .

HY-181102

TGR5 agonist 10	G protein-coupled Bile Acid Receptor 1	Metabolic Disease Inflammation/Immunology
TGR5 agonist 10 is a selective, allosteric and orally active Takeda G protein coupled receptor 5 (TGR5) agonist with EC₅₀s of 0.8 μM and 0.6 μM for human TGR5 and mouse TGR5, respectively. TGR5 agonist 10 demonstrates selectivity for TGR5 over FXR. TGR5 agonist 10 activates hTGR5 and mTGR5 to induce cAMP accumulation, and positively modulates lithocholic acid functional activity and potency at hTGR5, with higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 exerts glucose-lowering effects in Mus musculus oral glucose tolerance tests. TGR5 agonist 10 can be used for the research of diabetes .

HY-183692

FXR agonist 18	FXR G protein-coupled Bile Acid Receptor 1 TNF Receptor Heme Oxygenase (HO) Quinone Reductase Keap1-Nrf2	Cardiovascular Disease Inflammation/Immunology
FXR agonist 18 is an orally active FXR agonist, with an EC₅₀ of 10 nM against human FXR and an EC₅₀ of 1360 nM against human *TGR5. FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1, upregulating the expression of FXR, Hmox1, Nqo1, Nrf2*, and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis .

HY-41333

6ECA	G protein-coupled Bile Acid Receptor 1	Metabolic Disease
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 .

HY-182582

ZY12201	G protein-coupled Bile Acid Receptor 1 Cytochrome P450	Metabolic Disease
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 .

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P704194

	GPBAR1 Protein, Human (Cell-Free, His) G-protein coupled receptor GPCR19; hGPCR19; Membrane-type receptor for bile acids; M-BAR; hBG37; BG37; GPBAR1; TGR5	Human	E. coli Cell-free
	GPBAR1 Protein, Human (Cell-Free, His) is the recombinant human-derived GPBAR1 protein, expressed by E. coli cell-free system, with N-10*His tag.

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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