AM1241

製品コードS1544 バッチS154401

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H22IN3O3
分子量 503.33 CAS No. 444912-48-5
Solubility (25°C)* 体外 DMSO 101 mg/mL (200.66 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
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.
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
in vitro AM-1241 is a protean agonist of CB2 based on the different effect observed in various assays (calcium influx, extracellular signal-regulated kinase (ERK) phosphorylatin and cAMP measurement)) and on the switch from neutral antagonism to agonism in the cAMP assay when forskolin concentration is lowered. In [3H]CP 55,940 competition binding assays, this compound displays high affinity at the human CB2 receptor with a Ki value of about 7 nM, whereas its affinity at the human CB1 receptor is more than 80-fold weaker, using membrane preparations from stable HEK and CHO cell lines expressing the recombinant human CB2 and CB1 receptors, respectively. [2]
in vivo AM-1241 dose-dependently reverses tactile and thermal hypersensitivity produced by ligation of the L5 and L6 spinal nerves in rats. This compound is also active in blocking spinal nerve ligation-induced tactile and thermal hypersensitivity in mice lacking CB1 receptors (CB1-/- mice), confirming that it reverses sensory hypersensitivity independent of actions at CB1 receptors.[1] This chemical (100, 330 μg/kg i.p.) suppresses the development of carrageenan-evoked thermal and mechanical hyperalgesia and allodynia. And this suppression is blocked by CB2 antagonist SR144528 but not by CB1 antagonist SR141716A. [3] It produces dose-dependent antinociception to a thermal stimulus applied to the hindpaw, when administered into the hindpaw on the side of testing (ipsilateral i. paw), while much less active into the contralateral to the side. A50 (analgesic dose yielding a 50% effect) of this compound is 847 μg/kg with the maximum possible effect (100% MPE) being achieved at 3.3 mg/kg. It also produces dose-dependent antinociception when administered intraperitoneally (i.p.), with an A50 of 103μg/kg. The antinociceptive actions of this chemical are blocked by the CB2 receptor-selective antagonist AM630, but not by the CB1 receptor-selective antagonist AM251. This compound dosn't produce the CNS cannabinoid effects of hypothermia, catalepsy, inhibition of activity or impaired ambulation, while this tetrad of effects is produced by the mixed CB1/CB2 receptor agonist WIN55,212-2.[4] Daily injections of this chemical through a i.p. route, initiated at symptom onset, increases the survival interval after amyotrophic lateral sclerosis (ALS) onset by 56% in a transgenic mouse model of ALS. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Binding Assays
Binding to cannabinoid receptors is tested by using competition-equilibrium binding vs. [3H]CP55,940. AM-1241 is diluted into 25 mM Tris base (pH 7.4)/5 mM MgCl2/1 mM EDTA/0.1% essentially fatty acid-free BSA and transferred to Regisil-treated 96-well plates. [3H]CP55,940 (DuPont_NEN; specific activity 100–180 Ci/ mmol; 1 Ci =37 GBq) is added to a concentration of 0.8 nM. Membranes prepared from rat brain (containing CB1 receptors) or mouse spleen (containing CB2 receptors) are added (≈50 μg of membrane protein per well), plates are incubated at 30 °C for 1 hour, and the contents are filtered over Packard Unifilter GF/B 96-well filters by using a Packard Filtermate 196 cell harvester. Filters are washed with ice-cold 50 mM Tris base/5 mM MgCl2/0.5% BSA and dried. Bound radioactivity is quantitated and corrected for nonspecific binding, and results are normalized between 0% and 100% [3H]CP-55,940 specifically bound. IC50 is determined by nonlinear regression analysis using GraphPad PRISM and transformed to a Ki value. All data are collected in duplicate. IC50 and Ki values are determined from three independent experiments.
細胞アッセイ 細胞株 HEK cells and CHO cell lines stably express human CB2 receptor and CB1 receptor.
濃度 12 concentrations between 0.1 nM–10 μM
反応時間 90 minutes
実験の流れ Membrane samples are prepared from HEK cells stably expressing the human CB2 receptors previously generated (Mukherjee et al., 2004), or the CHO cell line that stably expresses the human CB1 receptor. Radioligand binding assays are performed as following. Briefly, the cells are harvested and homogenized using a Polytron for 2 × 10 s bursts in a buffer containing 50 mM Tris-HCl, pH 7.4, 1 mM MgCl2, and 1mM EDTA in the presence of protease inhibitors followed by centrifugation at 45 000 g for 20 minutes. The membrane pellets are washed and frozen at -80 °C in aliquots until use. Saturation binding reactions are performed at 30 °C for 90 minutes using [3H]CP 55,940 (0.01–8 nM) in an assay buffer containing 50 mM Tris-HCl, pH 7.4, 2.5 mM EDTA, 5mM MgCl2, and 0.05% fatty acid free bovine serum albumin (BSA) and the reactions are terminated by rapid vacuum filtration through UniFilter-96 GF/C filter plates and four washes with cold assay buffer. Competition experiments are conducted using 0.5 nM [3H]CP 55,940 in the presence of test compounds (0.1 nM–10 μM). Nonspecific binding is defined by 10 mM unlabeled CP 55,940. KD values from saturation binding assays and Ki values from competition binding assays are determined with one site binding or one site competition curve fitting using the Prism software.
動物実験 動物モデル 250-350 g male Sprague-Dawley rats
投薬量 0, 100, 300, 1000, 3000 μg/kg
投与方法 Administered via i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/12917492/
  • https://pubmed.ncbi.nlm.nih.gov/16894349/
  • https://pubmed.ncbi.nlm.nih.gov/12809695/
  • https://pubmed.ncbi.nlm.nih.gov/11514083/
  • https://pubmed.ncbi.nlm.nih.gov/17241118/

カスタマーフィードバック

Data from [Sci China Life Sci, 2014, 57(2), 201-8]

Data from [Data independently produced by , , Cell Physiol Biochem, 2016, 39(4):1521-36]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Cannabinoid CB2 receptor controls chronic itch by regulating spinal microglial activation and synaptic transmission [ Cell Rep, 2025, 44(4):115559] PubMed: 40222011
Cannabinoid Receptors CB1 and CB2 Activation Restores Hippocampal Lipid Profiles and Alleviates Autism-Like Behaviors in Valproic Acid-Induced ASD Rats [ CNS Neurosci Ther, 2025, 31(8):e70591] PubMed: 40852923
Therapeutic potential of EVs loaded with CB2 receptor agonist in spinal cord injury via the Nrf2/HO-1 pathway [ Redox Rep, 2024, 29(1):2420572] PubMed: 39466990
CB2R activation ameliorates late adolescent chronic alcohol exposure-induced anxiety-like behaviors during withdrawal by preventing morphological changes and suppressing NLRP3 inflammasome activation in prefrontal cortex microglia in mice [ Brain Behav Immun, 2023, 110:60-79] PubMed: 36754245
EVs-mediated delivery of CB2 receptor agonist for Alzheimer's disease therapy [ Asian J Pharm Sci, 2023, 18(4):100835] PubMed: 37645682
EVs-mediated delivery of CB2 receptor agonist for Alzheimer's disease therapy [ Asian J Pharm Sci, 2023, 18(4):100835] PubMed: 37645682
Activation of cannabinoid receptor 2 attenuates Angiotensin II-induced atrial fibrillation via a potential NOX/CaMKII mechanism [ Front Cardiovasc Med, 2022, 9:968014] PubMed: 36312282
Fast-Acting and Receptor-Mediated Regulation of Neuronal Signaling Pathways by Copaiba Essential Oil. [ Int J Mol Sci, 2020, 21(7)] PubMed: 32218156
The fatty-acid amide hydrolase inhibitor URB597 inhibits MICA/B shedding [ Sci Rep, 2020, 10(1):15556] PubMed: 32968163
Pharmacological activation of CB2 receptor protects against ethanol-induced myocardial injury related to RIP1/RIP3/MLKL-mediated necroptosis [ Mol Cell Biochem, 2020, 10.1007/s11010-020-03828-1] PubMed: 32681290

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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