HUMAN RECOMBINANT GPR142 RECEPTOR

MULTISCREEN™ DIVISION ARRESTED CELL LINE

Product Information

Catalog Number:
DC1286

Lot Number:
08/21/13

Quantity:
1 vial (4 x 106) frozen cells

Freeze Medium:
Sigma Freezing Medium (C-6164)

Host cell:
HEK293T

Transfection:
Expression vector containing full-length human GPR142 cDNA (GenBank Accession Number NM_181790.1) with FLAG tag sequence at N-terminus

Recommended Storage:
Liquid nitrogen upon receiving

Propagation Medium: DMEM, 10% FBS

Stability:
Stable in culture for 1-2 days after thawing

Data Sheet

Background: GPR142 belongs to the family of class A (rhodopsin-like) orphan G protein-coupled receptors. Research has linked GPR142 to type 2 diabetes mellitus. GPR142 is reported to be highly expressed in pancreatic β-cells, and upon ligand binding and also in the presence of a high concentration of blood glucose, can stimulate insulin secretion. It has been hypothesized that GPR142 agonists can provide a benefit over existing type 2 diabetes therapies because of a greatly reduced risk of hypoglycemia.

Application: Functional assays

Figure 1. Dose response of intracellular IP1 accumulation upon treatment with ligand, measured with IP-one Tb kit (Cisbio 62IPAPEC).

References:

Fredriksson R et al. (2003). “Seven evolutionarily conserved human rhodopsin G protein coupled receptors lacking close relatives”. FEBS Lett 554(3):381-8.

Lizarzaburu M et al. (2012). “Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus”. Bioorganic & Medicinal Chemistry Letters

FOR RESEARCH USE ONLY.
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