GPCR19
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.TGR5 gene locates on chromosome position 2q35 in humans. Its open reading frame has 993 base pairs, encoding 330 amino acids. High levels of TGR5 mRNA were detected in several organs such as small intestine, stomach, liver, lung, especially placenta and spleen. TGR5 can be activated by bile acids and then it induces cAMP production. As a membrane receptor, TGR5 can be internalized into the cytoplasm in response to its ligands. TGR5 plays important roles in cell signaling pathways such as nuclear factor κB (NF-κB), AKT, and extracellular signalregulated kinases (ERK). Its agonists may be potential drugs for treatment of metabolic, inflammation and digestive disorders. Activation of TGR5 has shown promise in treating various metabolic diseases such as type 2 diabetes (T2D) and obesity. Its activation also mediates novel effects on inflammation and cancer in different organs.
References
1.Guo C, et al. Front Physiol. 2016;7:646.
References
1.Guo C, et al. Front Physiol. 2016;7:646.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(471)
Bombesin Receptor(11)
Bradykinin Receptor(18)
Calcium Channel(137)
cAMP(9)
Cannabinoid Receptor(69)
CaSR(17)
CGRP Receptor(14)
Chemokine Receptor(104)
Cholecystokinin Receptor(17)
CRF Receptor(13)
Dopamine Receptor(145)
Endothelin Receptor(20)
FFAR(5)
Galanin Receptor(1)
GHSR(16)
Glucagon Receptor(36)
GPCR19(7)
GPR119(3)
Hedgehog (Hh)(27)
Histamine Receptor(110)
Imidazoline Receptor(1)
Leukotriene Receptor(9)
LHR(1)
LPA Receptor(12)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(6)
Melanocortin Receptor(22)
Melatonin Receptor(5)
mGluR(11)
Motilin Receptor(4)
Neurokinin Receptor(34)
Neuropeptide Y Receptor(36)
Neurotensin Receptor(8)
Orexin Receptor(14)
Other Targets(3)
OXTR(2)
P2Y Receptor(8)
PAR(24)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(60)
PTH Receptor(1)
S1P Receptor(22)
SGLT(22)
Somatostatin Receptor(11)
Urotensin Receptor(4)
Vasopressin Receptor(16)
GPCR19
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TC-G 1005
catalog no : M22970
cas no: 1415407-60-1
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. -
BAR 501 impurity
catalog no : M22739
cas no: 1632118-70-7
BAR501 impurity is an impurity found in the preparation of BAR501 that acts as an agonist of the G protein-coupled bile acid-activated receptor (GP-BAR1).? -
BAR502
catalog no : M21833
cas no: 1612191-86-2
BAR502 is a truncated side chain alcohol with both substituents on ring B in α-configuration. -
SBI-115
catalog no : M20784
cas no: 882366-16-7
SBI-115 is an?antagonist of?TGR5.?SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5. -
SMI-16a
catalog no : M17550
cas no: 587852-28-6
PIM1/2 Kinase Inhibitor VI, a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM).