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A-967079

A-967079

产品编号 T7205   CAS 1170613-55-4
别名: (1E,3E)-1-(4-氟苯基)-2-甲基-1-戊烯-3-酮肟

A 967079是一种有效的TRPA1受体选择性拮抗剂,对人和大鼠 TRPA1 受体的IC50分别为 67 nM 和 289 nM。A 967079具有良好的CNS 穿透性。

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A-967079 Chemical Structure
A-967079, CAS 1170613-55-4
规格 价格/CNY 货期 数量
1 mg ¥ 218 现货
5 mg ¥ 485 现货
10 mg ¥ 755 现货
25 mg ¥ 1,650 现货
50 mg ¥ 2,910 现货
100 mg ¥ 4,290 现货
1 mL * 10 mM (in DMSO) ¥ 530 现货
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产品目录号及名称: A-967079 (T7205)
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纯度: 100%
纯度: 98.34%
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参考文献
产品描述 A 967079 is a potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC50 values of 67 and 289 nM for the human and rat isoforms, respectively.
靶点活性 TRPA1 receptor (human):67 nM (IC50), TRPA1 receptor (rat):289 nM (IC50)
体内活性 Systemic injection of A 967079 (30 micromol/kg) decreased the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation of the ipsilateral hind paw in uninjured and CFA-inflamed rats. Similarly, A-967079 reduced the responses of WDR neurons to high-intensity mechanical stimulation (300 g von Frey hair) of the knee joint in both OA and OA-sham rats. WDR neuronal responses to low-intensity mechanical stimulation (10 g von Frey hair) were also reduced by A-967079 administration to CFA-inflamed rats, but no effect was observed in uninjured rats. Additionally, the spontaneous activity of WDR neurons was decreased after A-967079 injection in CFA-inflamed rats but was unaltered in uninjured, OA, and OA-sham animals[1].
动物实验 Separated by 5 min each, to specific stimulation of the neuronal RF were recorded. Spontaneous and evoked neuronal activity was then measured 5, 15, 25, and 35 min after systemic injection of A-967079 (30 μmol/kg) or vehicle (polyethylene glycol). The intravenous injection of A-967079 or vehicle was completed over a 6-7 min period. The i.v. dose of A-967079 was selected based on extrapolated plasma levels that were effective in behavioral studies . Except for 2 experiments in which two easily distinguished neurons were simultaneously recorded on one electrode, only one neuron was studied per rat. Since only one vehicle was used in these experiments, vehicle data was combined when a clear "no effect' was observed in at least 2-3 animals from a particular subset of groups (OA and sham OA)[1].
别名 (1E,3E)-1-(4-氟苯基)-2-甲基-1-戊烯-3-酮肟
分子量 207.24
分子式 C12H14FNO
CAS No. 1170613-55-4

存储

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

溶解度

DMSO: 100 mg/mL (482.53 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 4.8253 mL 24.1266 mL 48.2532 mL 120.6331 mL
5 mM 0.9651 mL 4.8253 mL 9.6506 mL 24.1266 mL
10 mM 0.4825 mL 2.4127 mL 4.8253 mL 12.0633 mL
20 mM 0.2413 mL 1.2063 mL 2.4127 mL 6.0317 mL
50 mM 0.0965 mL 0.4825 mL 0.9651 mL 2.4127 mL
100 mM 0.0483 mL 0.2413 mL 0.4825 mL 1.2063 mL

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TargetMol Library Books参考文献

1. McGaraughty S, Chu KL, Perner RJ,et al.TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats[J].Mol Pain. 2010 Mar 5;6:14. 2. Chen J , Joshi S K , Didomenico S , et al. Selective blocade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation[J]. Pain, 2011, 152(5):1165-1172.
TRPV4 agonist-1 free base AMTB hydrochloride AM12 TC-I2000 TRPM4-IN-1 Caffeic Acid 1,4-Cineole M084

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 膜蛋白靶向化合物库 NO PAINS 化合物库 血脑屏障通透化合物库 抗癌化合物库 经典已知活性库 已知活性化合物库 离子通道库 神经信号分子库

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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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Keywords

A-967079 1170613-55-4 Membrane transporter/Ion channel TRP/TRPV Channel TRP Channel inhibit Transient receptor potential channels A967079 A 967079 (1E,3E)-1-(4-氟苯基)-2-甲基-1-戊烯-3-酮肟 Inhibitor inhibitor

 

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