CB2R antagonist 3

Name: CB2R antagonist 3
Brand: MedChemExpress
SKU: HY-152581
Rating: 4.5 (1 reviews)

Cat. No.: HY-152581 Purity: 98.08%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines.

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

CB2R antagonist 3 Chemical Structure

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 480	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 480	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 437	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 656	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1313	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1970	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2955	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CB2R

In Vitro

CB2R antagonist 3 (compound 10a) (1 and 10 µM; 24 h) significantly reduces the TNF-α, IFN-γ, IL-1β, IL-6 pro-inflammatory cytokines expression and increases the IL-10 anti-inflammatory cytokines expression in monocytes and macrophages when combined with activator CB65 under the presence of lipopolysaccharide^[1].

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

Molecular Weight

410.64

Formula

C₂₇H₄₂N₂O

Appearance

Solid

Color

Light yellow to yellow

SMILES

CCCCCNC1=C(C=C(C=C1)CCCCC)C(NC23CC4CC(C3)CC(C2)C4)=O

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 : 100 mg/mL (243.52 mM; ultrasonic and warming and heat to 60°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	2.4352 mL	12.1761 mL	24.3522 mL
5 mM	0.4870 mL	2.4352 mL	4.8704 mL
10 mM	0.2435 mL	1.2176 mL	2.4352 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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: 2.5 mg/mL (6.09 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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 (25.0 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)

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

Purity: 98.08%

Select Batch:

Data Sheet (272 KB) SDS (0 KB)

COA (247 KB) HNMR (154 KB) RP-HPLC (145 KB) LCMS (393 KB)

Handling Instructions (2659 KB)

References

[1]. Graziano G, et al. N-adamantyl-anthranil amide derivatives: New selective ligands for the cannabinoid receptor subtype 2 (CB2R). Eur J Med Chem. 2023 Feb 15;248:115109. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4352 mL	12.1761 mL	24.3522 mL	60.8806 mL
	5 mM	0.4870 mL	2.4352 mL	4.8704 mL	12.1761 mL
	10 mM	0.2435 mL	1.2176 mL	2.4352 mL	6.0881 mL
	15 mM	0.1623 mL	0.8117 mL	1.6235 mL	4.0587 mL
	20 mM	0.1218 mL	0.6088 mL	1.2176 mL	3.0440 mL
	25 mM	0.0974 mL	0.4870 mL	0.9741 mL	2.4352 mL
	30 mM	0.0812 mL	0.4059 mL	0.8117 mL	2.0294 mL
	40 mM	0.0609 mL	0.3044 mL	0.6088 mL	1.5220 mL
	50 mM	0.0487 mL	0.2435 mL	0.4870 mL	1.2176 mL
	60 mM	0.0406 mL	0.2029 mL	0.4059 mL	1.0147 mL
	80 mM	0.0304 mL	0.1522 mL	0.3044 mL	0.7610 mL
	100 mM	0.0244 mL	0.1218 mL	0.2435 mL	0.6088 mL