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AM251 Cannabinoid Receptor antagonist

Name: AM251
Brand: Selleck Chemicals
SKU: S2819
Availability: InStock
Rating: 5 (12 reviews)

Cat.No.S2819

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

Chemical Structure

Molecular Weight: 555.24

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Quality Control

Batch: S281901 DMSO]40 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.02%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.02

Related Targets	K-Ras CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras
Other Cannabinoid Receptor Products	AM1241 BML-190 6-Iodopravadoline (AM630) Otenabant (CP-945598) HCl Org 27569 GW842166X WIN 55, 212-2 mesylate Pregnenolone monosulfate sodium RTICBM-189 Monlunabant

Solubility

In vitro
Batch:

DMSO : 40 mg/mL (72.04 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (1.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	555.24	Formula	C₂₂H₂₁Cl₂IN₄O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	183232-66-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I

Mechanism of Action

Features	A selective cannabinoid 1 blocker.
Targets/IC₅₀/Ki	CB1
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. This compound increases (by 2.3 times) the K_d of radioligand without altering B_max. It inhibits equilibrium binding by allosterically accelerating the dissociation of the [³H]-batrachotoxinin A 20-alpha-benzoate:sodium channel complex. This chemical reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2^+/+ and CB2 ^−/− peritoneal macrophages.
In vivo	AM251 causes a sustained reduction of daily food intake in the rat. This compound produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats. It disrupts memory consolidation of the inhibitory avoidance task. This chemical 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. It (4.0 mg/kg) reduces freezing during a conditioned tone cue played within a novel context.
References	[1] https://pubmed.ncbi.nlm.nih.gov/14748850/ [2] https://pubmed.ncbi.nlm.nih.gov/19338772/ [3] https://pubmed.ncbi.nlm.nih.gov/15451651/ [4] https://pubmed.ncbi.nlm.nih.gov/15948012/ [5] https://pubmed.ncbi.nlm.nih.gov/15721795/ [6] https://pubmed.ncbi.nlm.nih.gov/1646443/ [7] https://pubmed.ncbi.nlm.nih.gov/20347865/

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