2633686-53-8

2633686-53-8 structure

Name: CB1R Allosteric modulator 4
Chemical Name: CB1R Allosteric modulator 4
CAS Number: 2633686-53-8
Molecular Formula: C₂₀H₁₇N₃O₂S
Molecular Weight: 363.43
Catalog: Signaling Pathways GPCR/G Protein Cannabinoid Receptor
Create Date: 2022-10-11 18:06:41
Modify Date: 2024-09-19 20:12:47
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].

Name	CB1R Allosteric modulator 4

Description	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].
Related Catalog	Research Areas >> Others Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor
Target	hCB1-R
In Vitro	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].
References	[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 Med Chem. 2020 Nov 1;28(21):115727.

Molecular Formula	C₂₀H₁₇N₃O₂S
Molecular Weight	363.43