Cat.No. : CSC-RG01846 Host Cell: Human embryonic kidney immortal cell line (HEK293)
| Cat. No. | CSC-RG01846 |
| Description | This cell line is engineered to stably overexpress human glucagon like peptide 1 receptor (GLP1R) in HEK293 cells. |
| Gene | GLP1R |
| Gene Species | Homo sapiens (Human) |
| Host Cell | Human embryonic kidney immortal cell line (HEK293) |
| Host Cell Species | Homo sapiens (Human) |
| Stability | This cell line is stable at least 10 passages. |
| Product Type | Stable cell line constitutively expressing GPCR gene(s) |
| Applications | in vitro cell-based screening and discovery of GPCR agonists and antagonists |
| Quality Control | 1) GPCR activity assay 2) Mycoplasma detection |
| Size Form | One vial of frozen cells, typically >1x10^6cells/vial |
| Shipping | Dry ice |
| Storage | Liquid nitrogen |
| Resistance | Puromycin |
| Revival | Rapidly thaw cells in a 37°C water bath. Transfer contents into a tube containing pre-warmed media. Centrifuge cells and seed into a 25 cm2 flask containing pre-warmed media. |
| Growth Properties | Adherent |
| Mycoplasma | Negative |
| Format | One frozen vial containing millions of cells |
| Storage | Liquid nitrogen |
| Safety Considerations |
The following safety precautions should be observed. 1. Use pipette aids to prevent ingestion and keep aerosols down to a minimum. 2. No eating, drinking or smoking while handling the stable line. 3. Wash hands after handling the stable line and before leaving the lab. 4. Decontaminate work surface with disinfectant or 70% ethanol before and after working with stable cells. 5. All waste should be considered hazardous. 6. Dispose of all liquid waste after each experiment and treat with bleach. |
| Ship | Dry ice |
The incidence of diabetic cognitive impairment is increasing year by year and is gradually becoming a research hotspot. Studies have shown that glucagon-like peptide-1 receptor (GLP-1R) agonists can improve cognitive impairment in diabetic patients. Here, researchers explored whether small molecule GLP-1R agonists derived from traditional Chinese medicine could improve diabetic cognitive impairment. The study found that mollugin can bind to GLP-1R, promote Ca2+ influx in β-TC-6 cells, and increase insulin secretion and cAMP content. Mollugin also enhanced the viability of PC12 cells, reduced apoptosis, and lowered reactive oxygen species (ROS) levels in high glucose (HG)/hydrogen peroxide (H2O2)-damaged PC12 cells. Furthermore, mollugin shortened the escape latency in type 2 diabetic mice, improved neuronal damage, and reduced the expression of Pik3ca, Akt1, and Mapk1 mRNA in brain cortical tissue. These results suggest that mollugin may improve cognitive impairment in type 2 diabetic mice by activating the GLP-1R/cAMP/PKA signaling pathway.
Previous studies suggested that small molecules might have an affinity for GLP-1R, but it was not yet determined whether they were agonists or antagonists. To further confirm whether these small molecules could activate GLP-1R, researchers used calcium imaging technology to detect the effect of these small molecules on intracellular Ca2+ concentration in GLP1R Stable Cell Line - HEK293 (GLP-1R-HEK293) cells. Ca2+, as a second messenger, can reflect the binding of extracellular signals to cell surface receptors. The study showed that nobiletin, isosinensetin and mollugin can significantly promote calcium influx in GLP-1R-HEK293 cells (Figure 1A–G). To further determine the effect of these small molecules on GLP-1R, researchers measured their effect on insulin secretion in β cells. As shown in Figure 1H, these small molecules in 10 μM could promote insulin secretion by β cells in the presence of 1.38 mM glucose, as the positive drug liraglutide did, and the stimulatory effect of mollugin was the most significant. These preliminary results suggest that mollugin, isosinensetin and nobiletin may be GLP-1R agonists.
Figure 1. Calcium imaging of small molecules on GLP-1R-HEK293 cells. (Wang Z, et al., 2023)
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We adopted the Human GLP1R Stable Cell Line - HEK293 into our GPCR screening workflow and it’s been consistently reliable. Post-thaw recovery is smooth, signal windows in cAMP assays are robust with low background, and expression remains stable across passages.
Creative Biogene’s Human GLP-1R Stable Cell Line in HEK293 has delivered outstanding cAMP response curves with minimal background noise. The high expression level and rapid turnaround from thaw to assay made our drug screening pipeline far more efficient.
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