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Evaluation of LUXendin762 (CELT-113) distribution in vivo. (A) LUXendin762 (CELT-113, 200 nM) labels the membrane of SNAP-GLP1R:CHO-K1 cells (nuclei were stained using Hoechst33342) (scale bar = 40 μm) (n = 3 independent experiments). (B) Labeling efficiency of LUXendin762 (CELT-113) in SNAP-GLP1R:CHO-K1 cells (n = 5 wells). (C) LUXendin762 (CELT-113) is compatible with far-red SiR-tubulin that labels microtubules of SNAP-GLP1R:CHO-K1 cells (nuclei were stained using Hoechst33342; please note that not all cells were stained by SiR-tubulin) (scale bar = 10 μm). (D) LUXendin762 (CELT-113) is compatible with far-red SPY650-DNA that labels nuclei of SNAP-GLP1R:CHO-K1 cells (scale bar = 10 μm)
Evaluation of LUXendin762 (CELT-113) distribution in vivo. (E) In vivo images of mice intraperitoneally or subcutaneously injected with saline or LUXendin762 (CELT-113) at the baseline and 30 min and 1 h post-injection. Data plotted as the fold change of total radiant efficiency signals of the whole body measured at 30 min and 1 h post-injection. (F) Ex vivo analysis of harvested tissues 1 h post-intraperitoneal injection (n = 4 mice). (G) Ex vivo analysis of tissues 1 h post-subcutaneous injection (n = 4 mice). Graphs show mean ± SEM. #p = 0.08, *p < 0.05 (unpaired t-test for each tissue).

Our GLP1R fluorescent antagonist shows high affinity for GLP1 receptor (pIC50 = 7.0 for GLP1R) modulating the receptor by orthosteric antagonism. The efficacy and potency of LUXendin762 (CELT-113) as a GLP1R ligand was confirmed by a GLP-1 stimulated cAMP levels in SNAP-GLP1R:HEK293 cells. LUXendin762 (CELT-113) has been used in a variety of imaging applications, including widefield imaging in live and fixed mammalian cells and tissue. LUXendin762 is also compatible with non-invasive fluorescence preclinical imaging.

 

More information and applications

https://chemrxiv.org/engage/chemrxiv/article-details/60ff0d5a393cc904c94f1f18

LUXendin762 GLP1 receptor (GLP1R) fluorescent antagonist (762/784) (CELT-113)
For research use only

3 nmol vial that allows to prepare 30 µL of 100 µM stock solution to test GLP1R. One vial is sufficient for injecting one mouse.

Please note that the required concentration may vary depending on the specific assay design.

424,00€

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More information and contact in info@celtarys.com

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