CB1R Allosteric modulator 4_product_DataBase

Bioactivity	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].
Invitro	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].
Name	CB1R Allosteric modulator 4
CAS	2633686-53-8
Formula	C20H17N3O2S
Molar Mass	363.43
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]. 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

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