Product Details

Purity

Greater than 95% as determined by SDS-PAGE.

Endotoxin

Less than 1.0 EU/ug as determined by LAL method.

Activity

Measured by its binding ability in a functional ELISA. Immobilized human GCGR at 2 μg/mL can bind Anti-GCGR recombinant antibody (CSB-RA009316A1HU), the EC₅₀ is 3.747-6.666 ng/mL.

Target Names

GCGR

Uniprot No.

P47871

Research Area

Cancer

Alternative Names

GCGR; Glucagon receptor; GL-R

Molecular Characterization

Species

Homo sapiens (Human)

Source

Mammalian cell

Expression Region

26-136aa

Target Protein Sequence

AQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAK

Mol. Weight

18.1 kDa

Protein Length

Partial

Tag Info

N-terminal 10xHis-tagged and C-terminal Myc-tagged

Form

Lyophilized powder
Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.

Buffer

Lyophilized from a 0.2 μm filtered 20 mM Tris-HCl, 0.5 M NaCl, 6% Trehalose, pH 8.0

Reconstitution

We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. Our default final concentration of glycerol is 50%. Customers could use it as reference.

Troubleshooting and FAQs

Protein FAQs

Storage Condition

Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.

Shelf Life

The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.

Lead Time

3-7 business days

Notes

Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.

Datasheet & COA

Please contact us to get it.

Description

Mammalian cell-expressed recombinant human GCGR is a partial length protein tagged with a 10xHis motif at the N-terminus and a Myc motif at the C-terminus. Its DNA sequence corresponds to amino acids 26-136 of the human GCGR. This GCGR protein has high purity, greater than 95% determined by SDS-PAGE. It migrated to the molecular weight band of about 32 kDa on the gel. Its endotoxin content is less than 1.0 EU/ug measured by the LAL method. It is also biologically active and its activity has been validated through a functional ELISA by binding to the anti-GCGR antibody. And it is in stock now.

GCGR, a member of class B GPCR, combines with the natural ligand glucagon to regulate blood glucose homeostasis. It is an important drug target for type II diabetes. A series of drugs targeting GCGR have been developed to relieve hyperglycemia in diabetic patients, including GCGR antagonists, antibodies, and antisense oligonucleotides of GCGR.

Target Background

Function

G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system.

Gene References into Functions

3.0 A-resolution crystal structure of the full-length human glucagon receptor (GCGR) in complex with a glucagon analogue and partial agonist, NNC1702 PMID: 29300013
work toward the mapping of interactions between the polypeptide hormone glucagon and the glucagon receptor PMID: 28508109
3.0 A crystal structure of full-length GCGR containing both the extracellular domain and transmembrane domain in an inactive conformation PMID: 28514451
This work suggests that RAMP2 may modify the agonist activity and trafficking of the GCGR, with potential relevance to production of new peptide analogs with selective agonist activities. PMID: 28586439
Data suggest that GCGR activation proceeds via a mechanism in which transmembrane helix 6 (TM6) is held in an inactive conformation by a conserved polar core and a hydrophobic lock (involving intracellular loop 3, IC3); mutations in the corresponding polar core of GCGR disrupt these inhibitory elements, allow TM6 to swing outward, and induce constitutive G protein signaling. PMID: 28356352
The activation of the GCGR is characterized by the outward movement of the intracellular side of helix VI. In the active state of the GCGR, the Arg173(2.46)-Ser350(6.41) and Glu245(3.50)-Thr351(6.42) hydrogen bonds break, and the chi1 rotamer of Phe322(5.54) changes from perpendicular to parallel to helix VI. PMID: 27094704
In the glucagon receptor (GCGR) and glucagon-like peptide-1 receptor (GLP-1R), the extracellular domain is required for signaling even when the hormone is covalently linked to the transmembrane domain. PMID: 27226600
2.5 A crystal structure of human GCGR in complex with the antagonist MK-0893, which is found to bind to an allosteric site outside the seven transmembrane helical bundle in a position between TM6 and TM7 extending into the lipid bilayer PMID: 27111510
Molecular dynamics and disulfide crosslinking studies suggest that apo-GCGR can adopt both an open and closed conformation associated with extensive contacts between the ECD and 7TM domain. Glucagon binds to GCGR by a conformational selection mechanism. PMID: 26227798
glucagon cell adenomatosis with GCGR germline mutations seems to follow an autosomal-recessive trait. PMID: 25695890
Using a real-time time-resolved FRET-based internalization assay, we show that GLP-1R, GIPR, and GCGR internalize with differential properties PMID: 25451942
crystal structure of the seven transmembrane helical domain of human GCGR at 3.4 A resolution, and a hybrid model of glucagon bound to GCGR to understand the molecular recognition of the receptor for its native ligand PMID: 23863937
Letter/Case Report: nonfunctional glucagon cell adenomatosis with no detectable glucagon receptor mutations. PMID: 23407487
GRA1 is a potent glucagon receptor antagonist with strong antihyperglycemic efficacy in preclinical models and prominent effects on hepatic gene-expression related to amino acid metabolism PMID: 23185367
F22, V23, M27, and D15 of GCGR are the most important residues for glucagon binding. PMID: 22893257
in addition to activation of the classic cAMP/protein kinase A (PKA) pathway, activation of GCGR also induced beta-catenin stabilization and activated beta-catenin-mediated transcription PMID: 22438981
analysis of glucagon receptor antagonists with reduced molecular weight and lipophilicity PMID: 22119466
The P86S mutant GCGR shows abnormal receptor internalization & calcium mobilization, & causes apoptosis. It cases Mahvash disease (hyperglucagonemia, hypoglycemia, pancreatic neuroendocrine tumors). PMID: 21680267
substituted cysteine accessibility method and 3D-molecular modeling to study the N-terminal domain; results showed that Asp(63), Arg(116), and Lys(98) are essential for the receptor structure and/or ligand binding PMID: 20647307
The [Ca2+] response is induced by glucagon mainly via the coupling of GCGR to the Galphaq/11 and Galphai/o proteins. PMID: 19903011
The Gly40Ser polymorphism of the GCGR gene is associated with higher risk of hypertension and with enhanced proximal tubular sodium reabsorption. PMID: 11692154
Gly40Ser mutation in the glucagon receptor gene is not associated with type 2 diabetes in a Brazilian population, but a reduction of insulin secretion was observed in Gly40Ser carriers. PMID: 11961492
Three distinct epitopes on the extracellular face of the glucagon receptor determine specificity for the glucagon amino terminus PMID: 12724331
Expression of peroxisome proliferator-activated receptor gamma coactivator 1alpha (PGC-1alpha), known to be upregulated in the liver by fasting, was found to abolish the cAMP-dependent downregulation of glucagon receptor mRNA expression in vitro. PMID: 17374560

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Subcellular Location

Cell membrane; Multi-pass membrane protein.

Protein Families

G-protein coupled receptor 2 family

Database Links

HGNC: 4192

OMIM: 138033

KEGG: hsa:2642

STRING: 9606.ENSP00000383558

UniGene: Hs.208

Code	CSB-MP009316HU1
Abbreviation	Recombinant Human GCGR protein, partial (Active)
MSDS	MSDS Datasheet
Size	$136
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Image	(Tris-Glycine gel) Discontinuous SDS-PAGE (reduced) with 5% enrichment gel and 15% separation gel. Activity Measured by its binding ability in a functional ELISA. Immobilized human GCGR at 2 μg/ml can bind Anti-GCGR recombinant antibody (CSB-RA009316A1HU), the EC₅₀ is 3.747-6.666 ng/mL. Biological Activity Assay
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Recombinant Human Glucagon receptor (GCGR), partial (Active)

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