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AM1241

产品编号 T6755 CAS 444912-48-5

AM1241 是一种选择性大麻素 CB2 受体激动剂，Ki 为 3.4 nM，比 CB1 受体选择性高 82 倍。

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AM1241, CAS 444912-48-5

规格	价格/CNY	货期
2 mg	￥ 272	现货
5 mg	￥ 463	现货
10 mg	￥ 783	现货
25 mg	￥ 1,730	现货
50 mg	￥ 2,730	现货
100 mg	￥ 3,990	现货
500 mg	￥ 8,490	现货
1 mL * 10 mM (in DMSO)	￥ 912	现货

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其他形式的 AM1241:

(R)-AM1241
询价
(S)-AM1241
询价

选择批次

纯度: 98.82%

纯度: 98.72%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
靶点活性	CB2:3.4 nM(Ki)
体外活性	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, AM-1241 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]
体内活性	AM-1241 dose-dependently reverses tactile and thermal hypersensitivity produced by ligation of the L5 and L6 spinal nerves in rats. AM-1241 is also active in blocking spinal nerve ligation-induced tactile and thermal hypersensitivity in mice lacking CB1 receptors (CB1-/- mice), confirming that AM-1241 reverses sensory hypersensitivity independent of actions at CB1 receptors.[1] AM-1241 (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] AM1241 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 AM1241 is 847 μg/kg with the maximum possible effect (100% MPE) being achieved at 3.3 mg/kg. AM1241 also produces dose-dependent antinociception when administered intraperitoneally (i.p.), with an A50 of 103μg/kg. The antinociceptive actions of AM1241 are blocked by the CB2 receptor-selective antagonist AM630, but not by the CB1 receptor-selective antagonist AM251. AM1241 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 AM-1241 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]
激酶实验	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.
细胞实验	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 1 mM 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, 5 mM 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.(Only for Reference)

分子量	503.33
分子式	C22H22IN3O3
CAS No.	444912-48-5

存储

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

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (184.8 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9868 mL	9.9338 mL	19.8677 mL	49.6692 mL
	5 mM	0.3974 mL	1.9868 mL	3.9735 mL	9.9338 mL
	10 mM	0.1987 mL	0.9934 mL	1.9868 mL	4.9669 mL
	20 mM	0.0993 mL	0.4967 mL	0.9934 mL	2.4835 mL
	50 mM	0.0397 mL	0.1987 mL	0.3974 mL	0.9934 mL
	100 mM	0.0199 mL	0.0993 mL	0.1987 mL	0.4967 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Ibrahim MM, et al. Pro Natl Acad Sci USA, 2003, 100(18), 10529-10533. 2. Yao BB, et al, Br J Pharmacol, 2006, 149(2), 14-154. 3. Nackley AG, et al, Neuroscience, 2003, 119(3), 747-757. 4. Malan TP Jr, et al, Pain, 2002, 93(3), 239-245. 5. Shoemaker JL, et al, J Neurochem, 2007, 101(1), 87-98.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AM1241 444912-48-5 GPCR/G Protein Cannabinoid Receptor AM-1241 AM 1241 Inhibitor inhibitor inhibit

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AM1241

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords