| Bioactivity | CBR Agonist-1 (27a-cis) is a cannabinoid receptor (CBR) agonist with the Ki values of 0.18 μM for CB1R and 1.22 μM for CB2R. CBR Agonist-1 (27a-cis) can be used in the study of endogenous cannabinoid system-related diseases[1]. |
| Invitro | CBR Agonist-1 (27a-cis) (24 h) can activate GRABeCB2.0 (fluorescent CB1R sensor) in a concentration-dependent manner with the EC50 value of 2.1 μM in HEK293T cell lines[1].CBR Agonist-1 (27a-cis) (0-10 mM) acts on hCB1R calcium mobilization with the IC50 value of 3.10 μM in overexpressed hCB1R CHO-K1cells[1].CBR Agonist-1 (27a-cis) (10-1000 nM, 15 min) induces increased phosphorylation of extracellular signal-regulated kinases 1 and 2 (ERK1/2) in a dose-dependent manner in expressed Gαq16 and hCB1 CHO cells[1]. |
| Name | CBR Agonist-1 |
| Formula | C27H27FN4O |
| Molar Mass | 442.53 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Diego A Rodríguez-Soacha, et al. Development of an Indole-Amide-Based Photoswitchable Cannabinoid Receptor Subtype 1 (CB1R) "Cis-On" Agonist. ACS Chem Neurosci. 2022 Jul 26. |