CB1R Allosteric modulator 4 

CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment^[1].

CB1R is the most abundant G-protein coupled receptors (GPCR) in the CNS, CB1R involves in regulating physiological processes, from neurotransmission to energy metabolism^[1].
CB1R Allosteric modulator 4 (compound 66b) (0.10 nM-10µM; 30 min) exerts inhibition of forskolin-stimulated cellular cAMP production in CHO hCB1R with an EC₅₀ value of 0.05 μM^[1].
CB1R Allosteric modulator 4 (0.10 nM-10µM; 90 min) acts function for β-arrestin-2 recruitment in hCB1R-CHO-K1 cells with an EC₅₀ value of 0.163 μM^[1].
CB1R Allosteric modulator 4 (1.6-200 µM; 2 h) improves aqueous solubility with good biological activity, and shows kinetic water solubility with solubility limit of 3.13 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

363.43

C₂₀H₁₇N₃O₂S

2633686-53-8

O=[N+](CC(C1=NC=CS1)C2=C(C3=CC=CC=C3)NC4=C2C=CC(C)=C4)[O-]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Schaffer PC, et al. Focused structure-activity relationship profiling around the 2-phenylindole scaffold of a cannabinoid type-1 receptor agonist-positive allosteric modulator: site-III aromatic-ring congeners with enhanced activity and solubility. Bioorg  [Content Brief]