2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. AM-6538

AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability. AM-6538 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

AM-6538 Chemical Structure

AM-6538 Chemical Structure

CAS No. : 1245626-00-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 In-stock
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 690 In-stock
25 mg USD 1380 In-stock
50 mg USD 2200 In-stock
100 mg USD 3500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

AM-6538 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability[1]. AM-6538 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

cannabinoid[1]
In Vitro

AM6538 is a cannabinoid antagonist that binds CB1 receptors expressed in HEK-293 cells in a wash-resistant manner[1].

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

AM-6538 Related Antibodies
In Vivo

AM6538 (1~10 mg/kg) antagonizes the antinociceptive effects of cannabinoid agonists in mice[1].
AM6538 (10 mg/kg) shows that there are some recovery in the effects of AM4054. AM6538 dose dependently decreases the tau values for all cannabinoid agonists, reflecting reductions in the available receptors. AM6538 produces enduring antagonism, with robust effects on the tetrahydrocannabinol dose-effect function evident up to 7 days after treatment[1].

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

542.41

Formula

C26H25Cl2N5O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(C#CCCO[N+]([O-])=O)C=C3)=C1C)NN4CCCCC4
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 : 180 mg/mL (331.85 mM; Need ultrasonic; 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 1.8436 mL 9.2181 mL 18.4362 mL
5 mM 0.3687 mL 1.8436 mL 3.6872 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
×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 4.5 mg/mL (8.30 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 4.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (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)

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 1.8436 mL 9.2181 mL 18.4362 mL 46.0906 mL
5 mM 0.3687 mL 1.8436 mL 3.6872 mL 9.2181 mL
10 mM 0.1844 mL 0.9218 mL 1.8436 mL 4.6091 mL
15 mM 0.1229 mL 0.6145 mL 1.2291 mL 3.0727 mL
20 mM 0.0922 mL 0.4609 mL 0.9218 mL 2.3045 mL
25 mM 0.0737 mL 0.3687 mL 0.7374 mL 1.8436 mL
30 mM 0.0615 mL 0.3073 mL 0.6145 mL 1.5364 mL
40 mM 0.0461 mL 0.2305 mL 0.4609 mL 1.1523 mL
50 mM 0.0369 mL 0.1844 mL 0.3687 mL 0.9218 mL
60 mM 0.0307 mL 0.1536 mL 0.3073 mL 0.7682 mL
80 mM 0.0230 mL 0.1152 mL 0.2305 mL 0.5761 mL
100 mM 0.0184 mL 0.0922 mL 0.1844 mL 0.4609 mL
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AM-6538 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:

AM-65381245626-00-9AM6538AM 6538Cannabinoid Receptorlong-actingaffinitypseudo-irreversiblerimonabanttemporaryreductionsInhibitorinhibitorinhibit

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