TGR5 (GPCR19, GPR131, GPBAR1) (inhibitors, antagonists, agonists)-ProbeChem.com

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GPCR19, also known as G protein-coupled bile acid receptor 1 (GPBAR1) or TGR5, is a protein that in humans is encoded by the GPBAR1 gene. This gene encodes a member of the G protein-coupled receptor (GPCR) superfamily. This protein functions as a cell surface receptor for bile acids. Treatment of cells expressing this GPCR with bile acids induces the production of intracellular cAMP, activation of a MAP kinase signaling pathway, and internalization of the receptor. The receptor is implicated in the suppression of macrophage functions and regulation of energy homeostasis by bile acids.

Cat. No.	Product Name	Information
PC-20450	INT-777 TGR5 agonist	INT-777 (S-EMCA) is a potent, selective TGR5 agonist with EC50 of 0.82 uM.
PC-20449	SB-756050 TGR5 agonist	SB-756050 (SB756050) is a selective TGR5 agonist with EC50 of 1.3 uM (hTGR5), shows the potential for type 2 diabetes treatment.
PC-20448	TGR5 agonist 45h TGR5 agonist	TGR5 agonist 45h is a potent, selective and orally bioavailable TGR5 (GPBAR1) agonist with cAMP EC50 of 15 and 1 nM for hTGR5 and mTGR5, respectively.
PC-20447	BIX02694 TGR5 agonist	BIX02694 (BIX 02694) is a highly potent, in vivo-active TGR5 (GPBAR1) agonist with EC50 of 9 nM in AlphaScreen cAMP assays.
PC-20445	EX00000246 TGR5 agonist	EX00000246 is a highly potent TGR5 (GPBAR1) agonist with EC50 of 2 nM in AlphaScreen cAMP assays.
PC-20412	TGR5 agonist MN6 TGR5 agonist	TGR5 agonist MN6 is a potent and selective TGR5 agonist with cAMP EC50 values of 15.9 nM and 17.9 nM on hTGR5 and mTGR5, respectively.
PC-72133	ZY12201 TGR5 agonist	ZY12201 (TGR5 agonist 6g) is a highly potent, selective and orally efficacious TGR5 agonist with EC50 of 57 pM and 62 pM for hTGR5 and mTGR5, respectively.
PC-42345	BAR501 GPCR19 agonist	BAR501 is a potent, selective GPBAR1 (GPCR19, TGR5) agonist devoid of any FXR agonistic activity, effectively transactivates GPBAR1 in HEK293 cells with EC50 of 1 uM.
PC-20413	RDX8940 TGR5 agonist	RDX8940 (RDX009-01) is a potent, selective, minimally systemic oral TGR5 agonist.

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