Date published: 2025-10-25

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TGR5 Inhibitors

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.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

CHOLESTYRAMINE RESIN

11041-12-6sc-507509
5 g
$210.00
(0)

Cholestyramine binds to bile acids in the intestine, potentially reducing the availability of bile acids for TGR5 activation and thereby inhibiting its expression.

Guggulsterone

95975-55-6sc-203990
sc-203990A
10 mg
50 mg
$145.00
$615.00
1
(0)

Guggulsterone, a plant steroid found in guggul gum, has been shown to modulate bile acid receptor activity, which might influence TGR5 expression.

Fexaramine

574013-66-4sc-203580
sc-203580A
10 mg
50 mg
$398.00
$1380.00
1
(1)

Fexaramine is a synthetic farnesoid X receptor (FXR) agonist that indirectly regulates bile acid homeostasis, potentially impacting TGR5 expression.

GW 4064

278779-30-9sc-218577
5 mg
$93.00
13
(1)

GW4064 is another FXR agonist that may influence bile acid signaling and indirectly affect TGR5 expression.

Cyclosporin A

59865-13-3sc-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
(5)

Cyclosporin A has been shown to affect bile acid homeostasis, which might have an impact on TGR5 expression.

Rifampicin

13292-46-1sc-200910
sc-200910A
sc-200910B
sc-200910C
1 g
5 g
100 g
250 g
$95.00
$322.00
$663.00
$1438.00
6
(1)

Rifampicin has been shown to induce certain bile acid transporters and might influence TGR5 expression.

Troglitazone

97322-87-7sc-200904
sc-200904B
sc-200904A
5 mg
10 mg
25 mg
$108.00
$200.00
$426.00
9
(1)

Troglitazone, a PPAR-γ agonist, has been reported to modulate bile acid signaling and potentially affect TGR5 expression.

Rosiglitazone

122320-73-4sc-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
(1)

Rosiglitazone, another PPAR-γ agonist, might influence bile acid homeostasis and TGR5 expression.

Pioglitazone hydrochloride

112529-15-4sc-204848
sc-204848A
100 mg
500 mg
$62.00
$209.00
19
(2)

Pioglitazone hydrochloride is also a PPAR-γ agonist with potential effects on bile acid signaling and TGR5 expression.

Glyburide (Glibenclamide)

10238-21-8sc-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
(1)

Glibenclamide has been reported to interact with bile acid receptors and might influence TGR5 expression.