| 中文名称 |
A-836339
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| 英文名称 |
A-836339
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| 英文别名 |
CyclopropanecarboxaMide, N-[3-(2-Methoxyethyl)-4,5-diMethyl-2(3H)-thiazolylidene]-2,2,3,3-tetraMethyl-, [N(Z)]-;A-836339;1-(tetrahydropyran-4-ylMethyl)-1H-indol-3-yl]-(2,2,3,5-tetraMethylcyclopropyl)Methanone;[N(Z)]-N-[3-(2-Methoxyethyl)-4,5-dimethyl-2(3H)-thiazolylidene]-2,2,3,3-tetramethylcyclopropanecarboxamide (ACI);A 836339
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| Cas No. |
959746-77-1
|
| 分子式 |
C16H26N2O2S
|
| 分子量 |
310.45
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
|
| 详情描述 |
A-836339是CB2受体选择性激动剂,对CB1受体作用基本无。
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| 产品详情 |
A-836339是CB2受体选择性激动剂,对CB1受体作用基本无。
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| 生物活性 |
A-836339 is a cannabinoid CB2 receptor-selective agonist; exhibits high potencies at CB(2) and selectivity over CB(1) receptors.
IC50 value: 1.6 nM(EC50) [1]
Target: CB2 agonist
in vitro: In radioligand binding assays, A-836339 displays high affinities at CB(2) receptors and selectivity over CB(1) receptors in both human and rat.In addition A-836339 exhibits a profile devoid of significant affinity at other G-protein-coupled receptors and ion channels [1].
in vivo: In the complete Freunds adjuvant model of inflammatory pain, A-836339 exhibits a potent CB(2) receptor-mediated antihyperalgesic effect that is independent of CB(1) or mu-opioid receptors. A-836339 has also demonstrated efficacies in the chronic constrain injury (CCI) model of neuropathic pain, skin incision, and capsaicin-induced secondary mechanical hyperalgesia models [1]. Similar to systemic delivery, intra-
|
| 性状 |
Solid
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
Powder -20°C 3 years;4°C 2 years
|
| 参考文献 |
[1]. Yao BB, et al. Characterization of a cannabinoid CB2 receptor-selective agonist, A-836339 [2,2,3,3-tetramethyl-cyclopropanecarboxylic acid [3-(2-methoxy-ethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]-amide], using in vitro pharmacological assays, in vivo pa[2]. McGaraughty S, et al. A CB(2) receptor agonist, A-836339, modulates wide dynamic range neuronal activity in neuropathic rats: contributions of spinal and peripheral CB(2) receptors. Neuroscience. 2009 Feb 18;158(4):1652-61.
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| 溶解度数据 |
In Vitro: DMSO : 12 mg/mL (38.65 mM; Need ultrasonic and warming)配制储备液
|
[1]. Yao BB, et al. Characterization of a cannabinoid CB2 receptor-selective agonist, A-836339 [2,2,3,3-tetramethyl-cyclopropanecarboxylic acid [3-(2-methoxy-ethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]-amide], using in vitro pharmacological assays, in vivo pa[2]. McGaraughty S, et al. A CB(2) receptor agonist, A-836339, modulates wide dynamic range neuronal activity in neuropathic rats: contributions of spinal and peripheral CB(2) receptors. Neuroscience. 2009 Feb 18;158(4):1652-61.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。