1. GPCR/G Protein
    Neuronal Signaling
  2. Cannabinoid Receptor
  3. CB1/2 agonist 1

CB1/2 agonist 1 

Cat. No.: HY-147512
Handling Instructions

CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis.

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

CB1/2 agonist 1 Chemical Structure

CB1/2 agonist 1 Chemical Structure

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Description

CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis[1].

IC50 & Target[1]

hCB1-R

56.15 nM (EC50)

cannabinoid type-2 receptors

11.63 nM (EC50)

In Vitro

CB1/2 agonist 1 (compound B2) (10 µM) inhibits AEA hydrolysis with an IC50 of 5.9 µM for FAAH[1].
CB1/2 agonist 1 shows high affinity for CB1R and CB2R with Kis of 2.9, 1.5 nM, respectively[1].
CB1/2 agonist 1 (10 µM) shows anti-inflammatory effect and significantly decreases the secretion of IL-1β and IL-6, increases the release of anti-inflammatory IL-10 to 483.7% in LPS-activated BV-2 cells[1].
CB1/2 agonist 1 (1, 10 µM) inhibits 4-AP-evoked glutamate release[1].

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

In Vivo

CB1/2 agonist 1 (5-50 mg/kg) dose-dependently relieves neuropathic pain in a mouse model of oxaliplatin-induced neuropathic pain[1].

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

Molecular Weight

435.33

Formula

C21H24BrFN2O2

SMILES

CC1=C(C=C(C(N1CC2=CC=C(C=C2)F)=O)C(NC3CCCCCC3)=O)Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C1   V1   C2   V2

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Product Name:
CB1/2 agonist 1
Cat. No.:
HY-147512
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