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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
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 NO PAINS Compound Library Inhibitor Library GPCR Compound Library Anti-Fibrosis Compound Library Endocrinology-Hormone Compound Library Anti-Alzheimer's Disease Compound Library Bioactive Compound Library Bioactive Lipid Compound Library Neuronal Signaling Compound Library

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Keywords

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

 

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