coupled

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.

Linoleoyl Ethanolamide is an endocannabinoid agent. It acts by binding to TRPV1 increasing ERK phosphorylation and AP-1 dependent transcription in CB-receptor in an independent manner.

TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.

L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist and benzolactam derivative, known for reversing glucocorticoid-induced inhibition of GH secretion. L-692429 exhibits high affinity for the G protein-coupled receptor and is useful in studying acromegaly and obesity.

Ursodeoxycholic acid sodium (Sodium Ursodeoxycholate) is a naturally occurring secondary bile acid with anti-inflammatory and cytoprotective activities. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors,

Ursodeoxycholic acid (UDCA) is a potent inhibitor of liver-specific fatty acid transporter 5 (FATP5). Ursodeoxycholic acid inhibits cholesterol absorption and is used to dissolve gallstones.

Triamterene is a barosensitive epithelial sodium channel (ENaC) blocker with a diuretic effect. It can also act as an inhibitor of the TGR5 receptor, reducing GLP-1 secretion and cAMP level increases induced by TGR5 activation in a dose-dependent manner.

Deoxycholic acid (DCA) is a natural product and a TGR5 receptor agonist with cell permeability and oral activity. As a metabolite of intestinal flora, this compound is widely used in research on bile acid signal transduction, glucose and lipid metabolism, and anti-inflammatory mechanisms, and has shown therapeutic potential in diabetes and liver disease models.

Hyodeoxycholic acid (NSC 60672) has been used in trials studying the treatment of Hypercholesterolemia.

Deoxycholic acid sodium salt (Sodium deoxycholate) can activate the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

MBX-2982 is a selective, orally available GPR119 agonist used in the treatment of diabetes.

BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).

Fezagepras (Setogepram) is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84 with anti-inflammatory, anti-fibrotic, and anti-proliferative actions.

Anandamide ((5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide), an immune modulator, acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55) in the central nervous system.

GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.

Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83) that blocks recall in fear conditioning in mice. It exhibits inverse agonist and antagonist activity (Ki, 220 nM) at the A2A receptor and weak antagonist activity (Ki, 736 nM) at the 5-HT2B receptor.

TGR5 is a potent TGR5(GPCR19) agonist.

6-OAU (GTPL5846)(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

AS1269574 (AS 1269574) is a potent, orally available GPR119 agonist with potential for type 2 diabetes research.

CID 2745687 is a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50 = 6.70. CID 2745687 cannot effectively antagonize the agonist effects of either Zaprinast or Cromolyn disodium at rodent ortholog of GPR35 in vitro[1]. However, CID 2745687 can reverse lodoxamide-mediated anti-fibrotic effects in mice in vivo[2].

ML-193 (CID 1261822) is a potent and selective GPR55 antagonist (IC50: 221 nM) with over 27-fold selectivity for GPR55 over GPR35, CB1, and CB2. It can ameliorate motor and sensorimotor deficits in Parkinson's disease (PD) rats.

PSN 375963 (PSN 375963 hydrochloride) hydrochloride is a synthetic agonist of the endogenous ligand for GPR119.

GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.