计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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AM1241, CB 2 受体激动剂
有货
概述
AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.(R,S)-AM1241, a selective CB2 cannabinoid receptor agonist, has been used to study neuropathic pain in animal models
Information
AM-1241 is a selectivecannabinoid CB2 receptoragonist withKiof 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, 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.
In vivo
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. 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. 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. 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.
Cell Data
cell lines：
Concentrations：12 concentrations between 0.1 nM–10 μM
Incubation Time：90 minutes
Powder Purity:≥97%
规格
英文别名
(2-iodo-5-nitrophenyl)(1-((1-methylpiperidin-2-yl)methyl)-1H-indol-3-yl)methanone
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AM1241
生化机理
AM-1241 是一种选择性大麻素 CB2 受体激动剂，其Ki值为 3.4 nM，与 CB1 受体相比具有 82 倍的选择性。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激动剂
作用机制
CB 2 受体激动剂
名称和识别符
EC号
636-937-2
分子类型
小分子
Isomeric SMILES
CN1CCCCC1CN2C=C(C3=CC=CC=C32)C(=O)C4=C(C=CC(=C4)[N+](=O)[O-])I
关联CAS
MeSH Entry Terms
AM 1241;AM1241
分子量
503.33
Reaxy-Rn
10599020
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10599020&ln=
高级数据
关联靶点（人）
CNR2
Tchem
大麻素受体 2(Cannabinoid receptor 2)
(12 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 69 mg/mL (199.18 mM);
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H227: 可燃液体
预防措施声明
P210: 远离热源，热表面，火花，明火和其他点火源。 - 禁止抽烟。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P370+P378: 火灾时：使用干砂、干粉或抗醇泡沫灭火。
P403+P235: 存放在通风良好的地方。保持低温。
P501: 将内容物/容器送到批准的废物处理厂处理
WGK Germany
3
个人防护装备
dust mask type N95 (US)， Eyeshields， Faceshields， Gloves
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
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