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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, CAS 183232-66-8

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Purity: 98%

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	GPR55:39 nM, CB1:8 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 2 years

Solubility Information

Ethanol: 13.9 mg/mL (25 mM)

DMSO: 55.5 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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.

Citations

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

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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