CB1/2 agonist 4

CAS: 2772949-38-7 F: C27H45NO3 W: 431.65

CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB

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Bioactivity	CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively[1].
Target	Ki: 1.1 nM (hCB1); 4.2 nM (hCB2).EC50: 15.09 nM (CB1); EC50: 1.16 nM (CB2). IC50: 0.8 μM, EC50: 0.12 μM (TRPV1).
Invitro	CB1/2 agonist 4 (compound 24) has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively[1].CB1/2 agonist 4 (0.1 mM) can induce a stimulation of [35S]GTPγS binding to hCB1-CHO cell membranes with an EC50 value of 15.09 nM[1].CB1/2 agonist 4 (0.1 mM) is able to slightly stimulate [35S]GTPγS binding to hCB2-CHO cell membranes, behaving as a weak partial agonist to CB2 receptors of 1.16 nM[1].
In Vivo	CB1/2 agonist 4 (compound 24) (1, 3 and 4 mg/kg, i.p.) has a stronger antinociceptive activity[1].CB1/2 agonist 4 (1, 3 and 4 mg/kg, i.p.) can activate TRPV1 channel and it behaved as a good TRPV1 agonist with an IC50 value of 0.8 μM and EC50 value of 0.12 μM[1]. Animal Model:
Name	CB1/2 agonist 4
CAS	2772949-38-7
Formula	C27H45NO3
Molar Mass	431.65
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]. Antonella Brizzi, et al. Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity. Bioorg Med Chem. 2020 Jun 1;28(11):115513.

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