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(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
Urotensin Receptor(4)
Vasopressin Receptor(20)
GPCR19
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L-692429
产品货号 : M32989
cas no: 145455-23-8
L-692429 (MK-0751) 是一种苯并内酰胺的衍生物,也是一种非肽基生长激素促分泌素 (GHS) 激动剂。L-692429 以 Ki 值为 63 nM 来结合 G 蛋白偶联受体 (G protein-coupled receptor)。 -
INT-777
产品货号 : M32967
cas no: 1199796-29-6
INT-777是有效的 TGR5 激动剂,EC50 为 0.82 μM。 -
TC-G 1005
产品货号 : M22970
cas no: 1415407-60-1
TC-G 1005 是一种有效的选择性 GPBA 激动剂(EC50:0.72 nM;hTGR5)。对 TGR5 的选择性高于 FXR(法尼醇 X 受体)。增加小鼠血浆 GLP-1 水平并降低血糖。 -
BAR 501 impurity
产品货号 : M22739
cas no: 1632118-70-7
BAR501 杂质是在 BAR501 制备过程中发现的杂质,BAR501 充当 G 蛋白偶联胆汁酸激活受体 (GP-BAR1) 的激动剂。 -
BAR502
产品货号 : M21833
cas no: 1612191-86-2
BAR502 是一种 FXR 和 GPBAR1 双重激动剂,IC50 值分别为 2 μM 和 0.4 μM。