TGR5 inhibitors belong to a class of chemical compounds that specifically target and modulate the activity of the G protein-coupled receptor 5 (TGR5), also known as GPBAR1 (G protein-coupled bile acid receptor 1). TGR5 is a cell surface receptor found in various tissues throughout the human body, with a significant presence in the gastrointestinal tract, liver, and other organs. This receptor plays a crucial role in mediating the physiological effects of bile acids, which are essential molecules involved in the digestion and absorption of dietary fats. When bile acids bind to TGR5, it initiates a signaling cascade that can have various metabolic and immunomodulatory effects.
TGR5 inhibitors are designed to selectively block or modulate the activation of the TGR5 receptor. By doing so, they can interfere with the downstream signaling pathways triggered by TGR5 activation. This interference can lead to alterations in bile acid metabolism, immune responses, and metabolic processes in the body. TGR5 inhibitors have garnered significant interest in the field of pharmacology and drug development due to their ability to influence various physiological processes. Scientists continue to explore these inhibitors in the intricate role of TGR5 in human biology and its relevance in various health conditions.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
CHOLESTYRAMINE RESIN | 11041-12-6 | sc-507509 | 5 g | $210.00 | ||
Cholestyramine binds to bile acids in the intestine, potentially reducing the availability of bile acids for TGR5 activation and thereby inhibiting its expression. | ||||||
Guggulsterone | 95975-55-6 | sc-203990 sc-203990A | 10 mg 50 mg | $145.00 $615.00 | 1 | |
Guggulsterone, a plant steroid found in guggul gum, has been shown to modulate bile acid receptor activity, which might influence TGR5 expression. | ||||||
Fexaramine | 574013-66-4 | sc-203580 sc-203580A | 10 mg 50 mg | $398.00 $1380.00 | 1 | |
Fexaramine is a synthetic farnesoid X receptor (FXR) agonist that indirectly regulates bile acid homeostasis, potentially impacting TGR5 expression. | ||||||
GW 4064 | 278779-30-9 | sc-218577 | 5 mg | $93.00 | 13 | |
GW4064 is another FXR agonist that may influence bile acid signaling and indirectly affect TGR5 expression. | ||||||
Cyclosporin A | 59865-13-3 | sc-3503 sc-3503-CW sc-3503A sc-3503B sc-3503C sc-3503D | 100 mg 100 mg 500 mg 10 g 25 g 100 g | $62.00 $90.00 $299.00 $475.00 $1015.00 $2099.00 | 69 | |
Cyclosporin A has been shown to affect bile acid homeostasis, which might have an impact on TGR5 expression. | ||||||
Rifampicin | 13292-46-1 | sc-200910 sc-200910A sc-200910B sc-200910C | 1 g 5 g 100 g 250 g | $95.00 $322.00 $663.00 $1438.00 | 6 | |
Rifampicin has been shown to induce certain bile acid transporters and might influence TGR5 expression. | ||||||
Troglitazone | 97322-87-7 | sc-200904 sc-200904B sc-200904A | 5 mg 10 mg 25 mg | $108.00 $200.00 $426.00 | 9 | |
Troglitazone, a PPAR-γ agonist, has been reported to modulate bile acid signaling and potentially affect TGR5 expression. | ||||||
Rosiglitazone | 122320-73-4 | sc-202795 sc-202795A sc-202795C sc-202795D sc-202795B | 25 mg 100 mg 500 mg 1 g 5 g | $118.00 $320.00 $622.00 $928.00 $1234.00 | 38 | |
Rosiglitazone, another PPAR-γ agonist, might influence bile acid homeostasis and TGR5 expression. | ||||||
Pioglitazone hydrochloride | 112529-15-4 | sc-204848 sc-204848A | 100 mg 500 mg | $62.00 $209.00 | 19 | |
Pioglitazone hydrochloride is also a PPAR-γ agonist with potential effects on bile acid signaling and TGR5 expression. | ||||||
Glyburide (Glibenclamide) | 10238-21-8 | sc-200982 sc-200982A sc-200982D sc-200982B sc-200982C | 1 g 5 g 25 g 100 g 500 g | $45.00 $60.00 $115.00 $170.00 $520.00 | 36 | |
Glibenclamide has been reported to interact with bile acid receptors and might influence TGR5 expression. | ||||||