AM251

Catalog No.S2819

For research use only.

AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.

AM251 Chemical Structure

CAS No. 183232-66-8

Selleck's AM251 has been cited by 8 Publications

2 Customer Reviews

Purity & Quality Control

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Biological Activity

Description AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
Features A selective cannabinoid 1 blocker.
Targets
CB1 [2]
In vitro

AM251 reduces veratridine-dependent (tetrodotoxin suppressible) release of L-glutamic acid and GABA from synaptosomes with IC50 of 8.5 μM and 9.2 μM, respectively. AM251 increases (by 2.3 times) the Kd of radioligand without altering Bmax. AM251 inhibits equilibrium binding by allosterically accelerating the dissociation of the [3H]-batrachotoxinin A 20-alpha-benzoate:sodium channel complex. [1] AM251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2+/+ and CB2 −/− peritoneal macrophages. [2]

In vivo AM251 causes a sustained reduction of daily food intake in the rat. [3] AM251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats. [4] AM251 disrupts memory consolidation of the inhibitory avoidance task. [5] AM251 has caused a significative decrease in the test step-down latency when compared to the control group, but no differences are detected in the open field habituation task, including the number of crossings, i.e. there are no motor effects. [6] AM251 (4.0 mg/kg) reduces freezing during a conditioned tone cue played within a novel context. [7]

Protocol (from reference)

Animal Research:[5]
  • Animal Models: Moderately obese male Lewis rats
  • Dosages: 1.25 mg/kg, 2.5 mg/kg and 5 mg/kg
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 40 mg/mL
(72.04 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 555.24
Formula

C22H21Cl2IN4O

CAS No. 183232-66-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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