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HEK cells expressing the human CB1R labeled with (A) 10 µM CELT-335 and Hoechst 33342, (B) 3 µM CELT-335 and Hoechst 33342 and (C) 1 µM CELT-335 and Hoechst 33342, versus (D) 10 µM CELT-335 and Hoechst 33342 preincubated with 10 µM Rimonabant, (E) 3 µM CELT-335 and Hoechst 33342 preincubated with 10 µM Rimonabant and (F) 1 µM CELT-335 and Hoechst 33342 preincubated with 10 µM Rimonabant.
HEK cells expressing the human CB2R labeled with (A) 10µM CELT-335 and Hoechst 33342, (B) 3 µM CELT-335 and Hoechst 33342 and (C) 1 µM CELT-335 and Hoechst 33342, versus (D) 10 µM CELT-335 and Hoechst 33342 preincubated with 10 µM GW405833, (E) 3 µM CELT-335 and Hoechst 33342 preincubated with 10 µM GW405833 and (F) 1 µM CELT-335 and Hoechst 33342 preincubated with 10 µM GW405833.
Competition experiments of binding of fluorescent ligand CELT-335 to living HEK-293 T cells expressing the SNAP-CB1R. Tag-Lite® competition binding curves were obtained by using 100 nM of CELT-335 and increasing concentrations of compounds tested (0–10 μM). HTRF Ratio = 665 nm acceptor signal/620 nm donor signal × 10,000; the percentage is calculated by taking the highest value as 100%. Data represent the mean ± SEM (n = 5 in triplicates). (a) concentration/response curves obtained for agonists; (b) concentration/response curves obtained for the antagonists.
Competition experiments of binding of fluorophore-conjugated CELT-335 to living HEK-293 T cells expressing the CB1R. Competition binding experiments were performed in HEK-293 T cells transfected with 1 μg cDNA for SNAP-CB1R. Competition binding curves were obtained by HTRF using 100 nM of fluorophore- conjugated CELT-335 and increasing concentrations of Δ9-THC, Δ9-THCA and Δ9-THCV (0–10 μM). HTRF ratio = 665 nm acceptor signal/620 nm donor signal x 10,000; the percentage is calculated by taking the highest value as 100%. Data represent the mean ± SEM (n = 5 in triplicates).

Our CELT-335 product is a potent and selective hCB1/CB2 fluorescent ligand that shows a high affinity for CB1/CB2 receptors. It has a Ki value of 44.8 nM and 7.4 nM, respectively, in radioligand binding assay. CELT-335 has been validated in high-content screening assays and is also suitable for HTRF binding assays, providing a valid alternative to radioligand binding assays. It is available in a 10 µg vial that allows for the preparation of 150 mL of 100 nM working solution to test CB1R/CB2R. CELT-335 is designed to allow for cell visualization in fluorescence microscopy and is potentially suitable for other fluorescence-based assays.

More information and applications

Article 1: Similarities and differences upon binding of naturally occurring Δ9-tetrahydrocannabinol-derivatives to cannabinoid CB1 and CB2 receptors

Article 2: A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery

CELT-335 hCB1/CB2 cannabinoids receptors fluorescent ligand (646/662)
For research use only

10 µg vial can be used to prepare 72.58 µL of a 100 µM stock solution, providing enough volume for 7 assays at a working concentration of 100 nM.

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

476,00€

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More information and contact in info@celtarys.com

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