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

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.

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CB1/2 agonist 1 Chemical Structure

CB1/2 agonist 1 Chemical Structure

CAS No. : 2986688-90-6

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Based on 1 publication(s) in Google Scholar

CB1/2 agonist 1 Related Antibodies

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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].

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

CB1/2 agonist 1 Related Antibodies
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].

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

435.33

Formula

C21H24BrFN2O2
CAS No.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (45.94 mM; ultrasonic and warming and heat to 70°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2971 mL 11.4855 mL 22.9711 mL
5 mM 0.4594 mL 2.2971 mL 4.5942 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (4.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2971 mL 11.4855 mL 22.9711 mL 57.4277 mL
5 mM 0.4594 mL 2.2971 mL 4.5942 mL 11.4855 mL
10 mM 0.2297 mL 1.1486 mL 2.2971 mL 5.7428 mL
15 mM 0.1531 mL 0.7657 mL 1.5314 mL 3.8285 mL
20 mM 0.1149 mL 0.5743 mL 1.1486 mL 2.8714 mL
25 mM 0.0919 mL 0.4594 mL 0.9188 mL 2.2971 mL
30 mM 0.0766 mL 0.3829 mL 0.7657 mL 1.9143 mL
40 mM 0.0574 mL 0.2871 mL 0.5743 mL 1.4357 mL
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CB1/2 agonist 1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CB1/2 agonist 12986688-90-6Cannabinoid ReceptorBV-2 microglial cellanti-inflammatoryantinociceptiveIL-1βIL-10glutamate releasecross the blood-brain barrierInhibitorinhibitorinhibit

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