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

CB1 antagonist 2 (AM4113) is an orally active cannabinoid receptor type 1 (CB1R) antagonist. CB1 antagonist 2 suppresses appetite, reduces body weight, and blocks addictive behaviors such as heroin addiction, without causing adverse effects like nausea and depression that are associated with traditional CB1 inverse agonists. CB1 antagonist 2 can be used in studies related to obesity and opioid addiction.

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

CB1 antagonist 2

CB1 antagonist 2 Chemical Structure

CAS No. : 614726-85-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
250 mg In-stock
500 mg In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

CB1 antagonist 2 Related Antibodies

Top Publications Citing Use of Products

View All Cannabinoid Receptor Isoform Specific Products:

View All Isoforms
CB1 CB2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CB1 antagonist 2 (AM4113) is an orally active cannabinoid receptor type 1 (CB1R) antagonist. CB1 antagonist 2 suppresses appetite, reduces body weight, and blocks addictive behaviors such as heroin addiction, without causing adverse effects like nausea and depression that are associated with traditional CB1 inverse agonists. CB1 antagonist 2 can be used in studies related to obesity and opioid addiction[1][2][3].

In Vitro

CB1 antagonist 2 does not alter Forskolin (HY-15371)-stimulated cAMP formation in in vitro, indicating a lack of inverse agonist profile at CB1 receptors[2].

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

CB1 antagonist 2 Related Antibodies
In Vivo

CB1 antagonist 2 (0.3-5.6 mg/kg; i.p.; single administration) causes a dose-dependent reduction in locomotion and rearing behaviors in untreated adult male Sprague-Dawley rats at higher doses; at doses ≥1 mg/kg, it induces a dose-dependent increase in scratching and grooming behaviors in these rats[1].
CB1 antagonist 2 (0.3-3 mg/kg; i.p.; single administration) dose-dependently antagonizes WIN55,212-2-induced inhibition of spontaneous activity and rearing behavior, prolongation of latency, and circling behavior[1].
CB1 antagonist 2 (3-10 mg/kg; i.p.; single administration) dose-dependently inhibits heroin self-administration behavior in male Long-Evans rats. At i.p. doses of 3 mg/kg and 10 mg/kg, both the number of heroin infusions and active lever presses decrease with statistical significance[2].
CB1 antagonist 2 (2-10 mg/kg; i.p.; 14 days) causes a transient, dose-dependent reduction in food intake in rats, which in turn results in sustained, dose-dependent inhibition of body weight gain[3].
CB1 antagonist 2 (50 mg/kg; p.o.; 7 days) causes a sustained reduction in food intake in rats over 7 days, thereby significantly inhibiting body weight gain[3].

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

Animal Model: Sprague-Dawley (adult male, 2.5-3.5 months old)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: i.p.; single dose; co-administered with WIN55,212-2
Result: Completely reversed WIN55,212-2-induced suppression of ambulation to control levels at all three doses.
Partially reversed WIN55,212-2-induced suppression of rearing at all three doses, with levels significantly below controls but significantly higher than WIN55,212-2 alone.
Blocked WIN55,212-2-induced increases in latency to leave the center circle at all three doses.
Dose-dependently reduced WIN55,212-2-induced circling at all three doses.
Significantly increased scratching frequency at 1 mg/kg and 3 mg/kg compared to WIN55,212-2 alone.
Significantly increased grooming frequency and grooming duration at 3 mg/kg compared to WIN55,212-2 alone and controls.
Showed no significant effects on defecation, urination, or vocalization at any dose.
Animal Model: C57BL/6N (female, 10-16 weeks old, 20-30 g start weight; CB1 receptor knockout, wild-type)[3]
Dosage: 10 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced food intake at 2, 3, and 18 h post-administration in wild-type mice.
Produced no significant change in food intake compared to vehicle in CB1 receptor knockout mice.
Animal Model: Sprague-Dawley (male, 180-280 g start weight)[3]
Dosage: 2 mg/kg; 10 mg/kg
Administration: i.p.; daily; 14 days
Result: Significantly reduced food intake on treatment days 1 and 2 at 2 mg/kg, with body weight stabilizing at 5% less than vehicle-treated rats; body weight gain was significantly reduced on treatment days 5-14.
Significantly reduced food intake on treatment days 2-4 at 10 mg/kg, with body weight stabilizing at 10% less than vehicle-treated rats; body weight gain was significantly reduced on treatment days 5-14.
Reduced fat mass by 29.3±11.4% and lean body mass by 9.0±2.2% compared to vehicle-treated rats at 10 mg/kg, though differences did not reach statistical significance.
Showed no significant differences in plasma or hypothalamic 2-AG levels, or serum glucose, triglycerides, total cholesterol, or HDL cholesterol levels between AM4113-treated and vehicle-treated rats.
Molecular Weight

380.66

Formula

C17H12Cl3N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)C1=NN(C(C2=CC=C(C=C2)Cl)=C1C)C3=CC=C(C=C3Cl)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (164.19 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 2.6270 mL 13.1351 mL 26.2702 mL
5 mM 0.5254 mL 2.6270 mL 5.2540 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.08 mg/mL (5.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6270 mL 13.1351 mL 26.2702 mL 65.6754 mL
5 mM 0.5254 mL 2.6270 mL 5.2540 mL 13.1351 mL
10 mM 0.2627 mL 1.3135 mL 2.6270 mL 6.5675 mL
15 mM 0.1751 mL 0.8757 mL 1.7513 mL 4.3784 mL
20 mM 0.1314 mL 0.6568 mL 1.3135 mL 3.2838 mL
25 mM 0.1051 mL 0.5254 mL 1.0508 mL 2.6270 mL
30 mM 0.0876 mL 0.4378 mL 0.8757 mL 2.1892 mL
40 mM 0.0657 mL 0.3284 mL 0.6568 mL 1.6419 mL
50 mM 0.0525 mL 0.2627 mL 0.5254 mL 1.3135 mL
60 mM 0.0438 mL 0.2189 mL 0.4378 mL 1.0946 mL
80 mM 0.0328 mL 0.1642 mL 0.3284 mL 0.8209 mL
100 mM 0.0263 mL 0.1314 mL 0.2627 mL 0.6568 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CB1 antagonist 2 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 antagonist 2614726-85-1AM4113AM 4113AM-4113Cannabinoid ReceptorferretsCB1 receptor knockout miceCannabinoid 1 receptorobesityCB1Ropioid addictionratsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CB1 antagonist 2
Cat. No.:
HY-116649
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.