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Cat. No.: HY-150030

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CB1/2 agonist 4

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 K_i 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.

For research use only. We do not sell to patients.

CAS No.: 2772949-38-7
Formula: C₂₇H₄₅NO₃
Molecular Weight:431.65

Storage:

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

Data Sheet (266 KB)

CB1/2 agonist 4 Chemical Structure

CAS No.: 2772949-38-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Ki: 1.1 nM (hCB1); 4.2 nM (hCB2)^[1].
EC50: 15.09 nM (CB1); EC50: 1.16 nM (CB2)^[1].
IC50: 0.8 μM, EC50: 0.12 μM (TRPV1)^[1].

All Cannabinoid Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	1.16 nM Compound: 24	Agonist activity at human CB2 receptor expressed in CHO cell membrane assessed as inhibition of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay Agonist activity at human CB2 receptor expressed in CHO cell membrane assessed as inhibition of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	[PMID: 32340793]
CHO	EC₅₀	15.09 nM Compound: 24	Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	[PMID: 32340793]
HEK293	EC₅₀	0.12 μM Compound: 24	Activation of human TRPV1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay Activation of human TRPV1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay	[PMID: 32340793]
HEK293	EC₅₀	11.1 μM Compound: 24	Activation of rat recombinant TRPA1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay Activation of rat recombinant TRPA1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay	[PMID: 32340793]
HEK293	IC₅₀	>100 μM Compound: 24	Antagonist activity at rat recombinant TRPA1 expressed in HEK293 cells assessed as AITC-induced increase of calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay Antagonist activity at rat recombinant TRPA1 expressed in HEK293 cells assessed as AITC-induced increase of calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay	[PMID: 32340793]
HEK293	IC₅₀	0.8 μM Compound: 24	Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as capsaicin-induced increase of calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as capsaicin-induced increase of calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay	[PMID: 32340793]

In Vitro

CB1/2 agonist 4 (compound 24) has hCB1 and hCB2 receptor affinities with K_i 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].

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

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].

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

Animal Model:

Male CD-1 outbred mice^[1]
Dosage:

1, 3 and 4 mg/kg
Administration:

1, 3 and 4 mg/kg, i.p.
Result:

Significantly reduced the late phase of formalin-induced nociceptive behaviour in a dose dependent manner and slightly decreased also the first phase of nociceptive response.

Chemical Information

CAS No. 2772949-38-7
Molecular Weight 431.65
Formula C₂₇H₄₅NO₃
SMILES

O=C(NC1CC1)CCCCCCCOC2=CC(C(CCCCCC)(C)C)=CC(OC)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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