Recombinant Human G-Protein Coupled Bile Acid Receptor 1 (GPBAR1) Protein (His-KSI)

Name: Recombinant Human G-Protein Coupled Bile Acid Receptor 1 (GPBAR1) Protein (His-KSI)
Brand: Beta LifeScience
SKU: BLC-06682P
Availability: InStock

Greater than 85% as determined by SDS-PAGE.

Collections: High-quality recombinant proteins, Other recombinant proteins

Our products are highly customizable to meet your specific needs. You can choose options such as endotoxin removal, liquid or lyophilized forms, preferred tags, and the desired functional sequence range for proteins. Submitting a written inquiry expedites the quoting process.

Submit an inquiry today to inquire about all available size options and prices! Connect with us via the live chat in the bottom corner to receive immediate assistance.

Product Overview

Description	Recombinant Human G-Protein Coupled Bile Acid Receptor 1 (GPBAR1) Protein (His-KSI) is produced by our E.coli expression system. This is a protein fragment.
Purity	Greater than 85% as determined by SDS-PAGE.
Uniprotkb	Q8TDU6
Target Symbol	GPBAR1
Synonyms	(G-protein coupled receptor GPCR19)(hGPCR19)(Membrane-type receptor for bile acids)(M-BAR)(hBG37)(BG37)
Species	Homo sapiens (Human)
Expression System	E.coli
Tag	N-6His-KSI
Target Protein Sequence	GDQRYTAPWRAAAQRCLQGLWGRASRDSPGPSIAYHPSSQSSVDLDLN
Expression Range	283-330aa
Protein Length	Partial
Mol. Weight	20.6 kDa
Research Area	Others
Form	Liquid or Lyophilized powder
Buffer	Liquid form: default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol. Lyophilized powder form: the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose, pH 8.0.
Reconstitution	Briefly centrifuged the vial prior to opening to bring the contents to the bottom. Reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL. It is recommended to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. The default final concentration of glycerol is 50%.
Storage	1. Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. 2. Avoid repeated freeze-thaw cycles. 3. Store working aliquots at 4°C for up to one week. 4. In general, protein in liquid form is stable for up to 6 months at -20°C/-80°C. Protein in lyophilized powder form is stable for up to 12 months at -20°C/-80°C.
Notes	Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.

Target Details

Target Function	Receptor for bile acid. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production. May be involved in the suppression of macrophage functions by bile acids.
Subcellular Location	Cell membrane; Multi-pass membrane protein.
Protein Families	G-protein coupled receptor 1 family
Database References	HGNC: 19680 OMIM: 610147 KEGG: hsa:151306 STRING: 9606.ENSP00000428824 UniGene: PMID: 28916388 RYGB increased circulating bile acids, ileal Takeda G protein-coupled receptor 5 (TGR5) and mTORC1 signaling activity, as well as GLP-1 production in both mice and human subjects. Inhibition of ileal mTORC1 signaling by rapamycin significantly attenuated the stimulation of bile acid secretion, TGR5 expression and GLP-1 synthesis induced by RYGB in lean and diet-induced obese mice. PMID: 29859856 TGR5 is strongly expressed in collecting ducts, distal convoluted tubules and thin loop of Henle. TGR5 protein and mRNA expression were notably decreased in clear cell renal cell carcinomas and may be helpful in differentiating these tumors from other renal cell carcinomas. PMID: 29606134 The findings suggest that activation of TGR5 promoted mitochondrial biogenesis in endothelial cells, which is mediated by the CREB/PGC-1a signaling pathway. PMID: 29709472 Higher-order oligomers, likely with a tetramer organization, are formed from dimers, the smallest unit suggested for TGR5 Y111A variants. PMID: 27833095 Data suggest that TGR5 and FXR in intestinal mucosa are important for glucose homeostasis, in particular in metabolic disorders such as type 2 diabetes and obesity. (TGR5 = membrane-type receptor for bile acids TGR5; FXR = farnesoid X receptor) [REVIEW; Congress as Topic] PMID: 27846919 GPBAR1 is expressed in advanced gastric cancers and its expression correlates with markers of epithelial-mesenchymal transition PMID: 27409173 TGR5 activation induces mitochondrial biogenesis and prevents renal oxidative stress and lipid accumulation, establishing a role for TGR5 in inhibiting Kidney Disease in Obesity and Diabetes Mellitus. PMID: 27045028 TGR5 exhibits significantly higher expression in NSCLC tumor samples and facilitates the growth and metastasis of NSCLC by activating the JAK2/STAT3 signaling pathway. PMID: 29074425 TGR5 may have a role in the progression from Barrett's Esophagus to high-grade dysplasia and esophageal adenocarcinoma PMID: 28293080 contributes to hepatic cystogenesis by increasing cAMP and enhancing cholangiocyte proliferation PMID: 28543567 anti-inflammation therapy targeting Gpbar1/NF-kappaB pathway could be effective in suppressing bile acid-induced inflammation and alleviating Intrahepatic cholestasis of pregnancy-associated fetal disorders. PMID: 27402811 human TGR5 (hTGR5) shows higher nomilin responsiveness than does mouse TGR5. PMID: 28594916 bile acids promote intestinal epithelial cell proliferation and decrease mucosal injury by upregulating TGR5 expression in obstructive jaundice. PMID: 28034761 The generated contour maps revealed the important structural insights for the activity of the compounds. The results obtained from this study could be helpful in the development of novel and more potent agonists of TGR5. PMID: 27267434 TGR5 functions as a tumor-suppressor in patients with ampullary adenocarcinoma and preoperative hyperbilirubinemia PMID: 27510297 We conclude that Claudin-2 expression is significantly associated with bile acid receptors VDR and TGR5 expression. Our studies identify a novel role of a tight junction protein in the development and progression of esophageal mucosal metaplasia, dysplasia and carcinoma. PMID: 28212604 this is the first report of bile acid derivatives able to antagonize GPBAR1 and and farnesoid X receptor (FXR) modulatory activity. PMID: 26607331 These findings identify TGR5 as a suppressor of gastric cancer cell proliferation and migration PMID: 26417930 Because elevated levels of circulatory LPS may contribute to the development of insulin resistance, the results from this study suggest that bile acids through the activation of TGR5 may have a role in the development of insulin resistance as well. PMID: 25418122 TGR5 is a mediator of bile acid-induced cholangiocyte proliferation and protects cholangiocytes from apoptosis but may trigger proliferation and apoptosis resistance in malignantly transformed cholangiocytes, promoting cholangiocarcinoma. PMID: 26420419 Collectively, these data suggest the involvement of TGR5 in PLD and that TGR5 targeting in cystic cholangiocytes may have therapeutic potential. PMID: 26045278 GPBAR1 plays a role in secondary bile acid induced vasodilation via reglation of cystathionine gamma-lyase. The GPBAR1/CSE pathway might contribute to endothelial dysfunction and hyperdynamic circulation in liver cirrhosis. PMID: 25934094 Study demonstrates that highly lipophilic 3-epi-betulinic acid derivatives can be potent and selective TGR5 agonists with improved cellular efficacy. PMID: 25283506 GPBAR1 SNP is associated with symptoms and pathobiology in IBS-D and IBS-C. PMID: 25012842 Our findings strongly suggested the combination of serum TGR5 promoter methylation and AFP enhanced the diagnostic value of AFP alone in discriminating HCC from CHB patients. PMID: 24465162 the secondary structure of the TGR5 membrane-proximal C terminus is the determining factor for plasma membrane localization and responsiveness towards extracellular ligands. PMID: 24338481 Data suggest that TGR5 is expressed in 2 cell types of term placenta, macrophage/trophoblast; TGR5 expression is low in maternal cholestasis; TGR5 appears to trigger different responses to bile acid/progesterone metabolites depending on cell type. PMID: 23849932 DCA, taurolithocholic acid, and oleanolic acid did not stimulate TGR5 association with beta-arrestin 1/2 or G protein-coupled receptor kinase (GRK) 2/5/6, as determined by bioluminescence resonance energy transfer PMID: 23818521 TGR5 agonism induces NO production via Akt activation and intracellular Ca(2+) increase in vascular endothelial cells, and this function inhibits monocyte adhesion in response to inflammatory stimuli. PMID: 23619297 Human adipose tissue TGR5 expression is positively correlated to obesity and reduced during diet-induced weight loss. PMID: 23523790 TGR5 signalling inhibits the production of pro-inflammatory cytokines by in vitro differentiated inflammatory and intestinal macrophages in Crohn's disease. PMID: 23566200 TGR5 is overexpressed in most gastric intestinal-type adenocarcinomas, and moderate to strong TGR5 staining is associated with decreased patient survival in all gastric adenocarcinomas. PMID: 23238937 this study demonstrates that the TGR5 expressed in the pancreatic beta cells regulates insulin secretion and highlights the importance of ongoing therapeutic strategies targeting TGR5 in the control of glucose homeostasis. PMID: 23022524 the mechanisms of metabolic regulation by FXR and TGR5 PMID: 22550135 These results indicate that bile acids induce the differentiation of IL-12 hypo-producing dendritic cells from monocytes via the TGR5-cAMP pathway. PMID: 22236403 Data suggest that variation in bile acid receptor TGR5 may contribute to altered small bowel transit and colonic transit in lower functional gastrointestinal disorders. PMID: 21883702 TGR5 is a key factor in energy expenditure by regulating metabolism. PMID: 21754919 The current knowledge on BA receptors is reviewed, with a strong focus on the cell membrane receptor TGR5, which has emerged as a promising target for intervention in metabolic diseases. PMID: 21691102 The aim of the present study was to determine the localization and function of the receptor in biliary epithelial cells. PMID: 21691103 The TGR5 gene is localized at chromosome 2q35, close to a genetic variant associated with both primary sclerosing cholangitis and ulcerative colitis in recent genome-wide association studies. PMID: 21691110 The ability of the bile acid analogues obtained by chemical modification of ursodeoxycholic acid (UDCA) for TGR5 activation in HEK 293 cells is reported. PMID: 21212509 The TGR5 is localized in the primary cilium of human cholangiocytes and the receptor could play an important role in coupling biliary bile acid concentration and composition to ductular bile formation. PMID: 20623999 resequencing of TGR5 along with functional investigations of novel variants PMID: 20811628 Expression of BG37 was detected in various specific tissues, suggesting its physiological role. PMID: 12419312 TGR5 is implicated in the suppression of macrophage functions by bile acids PMID: 12524422 Combined blockade of both epidermal growth factor receptors and GPCRs may be a rational strategy to treat cancers, including head and neck squamous cell carcinoma that shows cross-talk between GPCR and EGFR signaling pathways. PMID: 17178880 These results suggest that in AGS cells, DC transactivates EGFR through M-BAR- and ADAM/HB-EGF-dependent mechanisms. PMID: 17214962 This is the first report on the expression of TGR5 in sinusoidal endothelial cells. Regulation of eNOS by TGR5 connects bile salts with hepatic hemodynamics. PMID: 17326144 TGR5 mediates chloride secretion via activation of CFTR. The presence of the receptor in both the plasma membrane and the recycling endosome indicate that TGR5 can be regulated by translocation. PMID: 19582812

FAQs

Please fill out the Online Inquiry form located on the product page. Key product information has been pre-populated. You may also email your questions and inquiry requests to sales1@betalifesci.com. We will do our best to get back to you within 4 business hours.

Feel free to use the Chat function to initiate a live chat. Our customer representative can provide you with a quote immediately.

Proteins are sensitive to heat, and freeze-drying can preserve the activity of the majority of proteins. It improves protein stability, extends storage time, and reduces shipping costs. However, freeze-drying can also lead to the loss of the active portion of the protein and cause aggregation and denaturation issues. Nonetheless, these adverse effects can be minimized by incorporating protective agents such as stabilizers, additives, and excipients, and by carefully controlling various lyophilization conditions.

Commonly used protectant include saccharides, polyols, polymers, surfactants, some proteins and amino acids etc. We usually add 8% (mass ratio by volume) of trehalose and mannitol as lyoprotectant. Trehalose can significantly prevent the alter of the protein secondary structure, the extension and aggregation of proteins during freeze-drying process; mannitol is also a universal applied protectant and fillers, which can reduce the aggregation of certain proteins after lyophilization.

Our protein products do not contain carrier protein or other additives (such as bovine serum albumin (BSA), human serum albumin (HSA) and sucrose, etc., and when lyophilized with the solution with the lowest salt content, they often cannot form A white grid structure, but a small amount of protein is deposited in the tube during the freeze-drying process, forming a thin or invisible transparent protein layer.

Reminder: Before opening the tube cap, we recommend that you quickly centrifuge for 20-30 seconds in a small centrifuge, so that the protein attached to the tube cap or the tube wall can be aggregated at the bottom of the tube. Our quality control procedures ensure that each tube contains the correct amount of protein, and although sometimes you can't see the protein powder, the amount of protein in the tube is still very precise.

To learn more about how to properly dissolve the lyophilized recombinant protein, please visit Lyophilization FAQs.