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AM251

Catalog No. T1915   CAS 183232-66-8

AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).

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AM251 Chemical Structure
AM251, CAS 183232-66-8
Pack Size Availability Price/USD Quantity
5 mg In stock $ 43.00
10 mg In stock $ 72.00
25 mg In stock $ 132.00
50 mg In stock $ 235.00
100 mg In stock $ 348.00
1 mL * 10 mM (in DMSO) In stock $ 64.00
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Purity: 97.88%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).
Targets&IC50 CB1:8 nM, GPR55:39 nM
In vitro AM251 inhibits memory consolidation in avoidance tasks. Compared to the control group, AM251 significantly reduces latency in tested subjects, yet no difference is observed in open field adaptive tasks, including the number of crossroads. In related fear memory tests, animals pre-treated with AM251 (4.0/8.0 mg/kg) exhibit enhanced rigidity. AM251 consistently decreases daily food intake in rats, induces selective feeding, and behaviors associated with nausea, without affecting the rate of consumption.
In vivo AM251 inhibits equilibrium binding by accelerating the dissociation of the [3H]-batrachotoxinin A 20-α-benzoate: sodium channel complex through a conformational change. It increases the dissociation constant (Kd) of the radioligand by 2.3 times without affecting the maximum binding capacity (Bmax). Furthermore, AM251 reduces the release of tetrodotoxin-inhibitory L-glutamate (IC50: 8.5 μM) and GABA (IC50: 9.2 μM) from synaptosomes in a veratridine-dependent manner. It also decreases unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, along with reducing the synthesis of cholesteryl esters in both CB2+/+ and CB2-/- peritoneal macrophages.
Kinase Assay Macrophages are seeded (2×106/well) in 12-well culture plates. AM-251 or SR144528 are added from 4 mM stock solutions prepared in DMSO, 1h prior to the addition of 7-ketocholesterol (7KC) from a 2 mg/mL ethanol stock solution. Controls are adjusted to receive equivalent volumes of DMSO and ethanol. After 16 h, caspase-3 activity is determined. All treatments are done in triplicate and the data presented as the mean RFLU/mg protein±SD[3].
Molecular Weight 555.24
Formula C22H21Cl2IN4O
CAS No. 183232-66-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 13.9 mg/mL (25 mM)

DMSO: 55.5 mg/mL (100 mM)

TargetMolReferences and Literature

1. Liao C, et al. Basic Clin Pharmacol Toxicol, 2004, 94(2), 73-78. 2. Thewke D, et al. Biochem Biophys Res Commun, 2009, 381(2), 181-186. 3. Chambers AP, et al. Physiol Behav, 2004, 82(5), 863-869. 4. McLaughlin PJ, et al. Psychopharmacology (Berl), 2005, 180(2), 286-293. 5. de Oliveira Alvares L, et al. Neurobiol Learn Mem, 2005, 83(2), 119-124. 6. Komaki A, et al. Study the Effect of Endocannabinoid System on Rat Behavior in Elevated Plus-Maze. Basic Clin Neurosci. 2015 Jul;6(3):147-53. 7. Carey LM, et al. A pro-nociceptive phenotype unmasked in mice lacking fatty-acid amide hydrolase. Mol Pain. 2016 May 13;12. pii: 1744806916649192. 8. Jiang X, et al. Role of cannabinoid receptor type 1 in tibial and pudendal neuromodulation of bladder overactivity in cats. Am J Physiol Renal Physiol. 2017 Mar 1;312(3):F482-F488. 9. Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814. 10. Bowden G D, Land K M, O'Connor R M, et al. High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth[J]. International Journal for Parasitology: Drugs and Drug Resistance. 2018 Apr;8(1): 137-144.

TargetMolCitations

1. Li P, Lin Q, Sun S, et al. Inhibition of cannabinoid receptor type 1 sensitizes triple-negative breast cancer cells to ferroptosis via regulating fatty acid metabolism. Cell Death & Disease. 2022, 13(9): 1-15. 2. Bowden G D, Land K M, O'Connor R M, et al. High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth. International Journal for Parasitology: Drugs and Drug Resistance. 2018 Apr;8(1): 137-144

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library GPCR Compound Library Inhibitor Library Membrane Protein-targeted Compound Library Anti-Alzheimer's Disease Compound Library Bioactive Compound Library Anti-Obesity Compound Library Endocrinology-Hormone Compound Library ReFRAME Related Library Target-Focused Phenotypic Screening Library

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Keywords

AM251 183232-66-8 Endocrinology/Hormones GPCR/G Protein GPR Cannabinoid Receptor Inhibitor AM 251 inhibit AM-251 inhibitor

 

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