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A-836339

A-836339

产品编号 T7375   CAS 959746-77-1

A-836339 是一种 CB2 受体选择性激动剂,对 CB1受体基本无作用。

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A-836339 Chemical Structure
A-836339, CAS 959746-77-1
规格 价格/CNY 货期 数量
1 mg ¥ 413 现货
5 mg ¥ 1,580 现货
10 mg ¥ 2,820 现货
25 mg ¥ 4,760 现货
50 mg ¥ 6,780 现货
100 mg ¥ 9,180 现货
1 mL * 10 mM (in DMSO) ¥ 1,730 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: A-836339 (T7375)
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纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 A-836339 acts as a potent cannabinoid receptor full agonist which has a higher affinity for the peripheral CB2 receptor (Ki = 0.64 nM) over the central CB1 receptor (Ki = 270 nM). It displays analgesic, anti-inflammatory, and anti-hyperalgesic effects in mice.
体内活性 A-836339 was characterized extensively in various animal pain models. In the complete Freund's 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. Furthermore, no tolerance was developed in the CCI model after subchronic treatment with A-836339 for 5 days[1].
动物实验 The plantar aspect of the rat left hind paw was exposed through a hole in a sterile plastic drape, and a 1-cm longitudinal incision was made through the skin and fascia, starting 0.5 cm from the proximal edge of the heel and extending toward the toes. The plantaris muscle was elevated and incised longitudinally, leaving the muscle origin and insertion points intact. After homeostasis by application of gentle pressure, the skin was apposed with two mattress sutures using 5-0 nylon. Animals were then allowed to recover for 2 or 24 h after surgery, at which time mechanical allodynia was assessed.To test drug effects, rats were first acclimated for 20 min in inverted individual plastic containers (20*12.5*20 cm) on top of a suspended wire mesh grid, and A-836339 was injected intraperitoneally 30 min before testing for mechanical allodynia using calibrated von Frey filaments . von Frey filaments were presented perpendicularly to the plantar surface of the selected hind paw and then held in this position for approximately 8 s, with enough force to cause a slight bend of the filament. Positive responses included an abrupt withdrawal of the hind paw from the stimulus or flinching behavior immediately after removal of the stimulus. A 50% withdrawal threshold was determined using an up-down procedure[1].
分子量 310.45
分子式 C16H26N2O2S
CAS No. 959746-77-1

存储

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

溶解度

DMSO: 12 mg/mL (38.65 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 3.2211 mL 16.1057 mL 32.2113 mL 80.5283 mL
5 mM 0.6442 mL 3.2211 mL 6.4423 mL 16.1057 mL
10 mM 0.3221 mL 1.6106 mL 3.2211 mL 8.0528 mL
20 mM 0.1611 mL 0.8053 mL 1.6106 mL 4.0264 mL

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TargetMol Library Books参考文献

1. 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 Pain Models, and Pharmacological Magnetic Resonance Imaging[J]. Journal of Pharmacology and Experimental Therapeutics, 2009, 328(1):141-151. 2. Mcgaraughty S , Chu K M , Yao B , 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[J]. Neuroscience, 2009, 158(4):1652-1661.
COR659 CB1 agonist 1 Rimonabant AM251 O-1602 PSNCBAM-1 MJ 15 GP 1a

相关化合物库

该产品包含在如下化合物库中:
膜蛋白靶向化合物库 GPCR靶点分子库 已知活性化合物库 神经信号分子库 NO PAINS 化合物库 经典已知活性库 抗纤维化化合物库 抗衰老化合物库

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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。

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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

A-836339 959746-77-1 GPCR/G Protein Cannabinoid Receptor A836339 inhibit Inhibitor A 836339 inhibitor

 

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