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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。
规格 | 价格 | 库存 | 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 x 10 mM (in DMSO) | ¥ 530 | 现货 |
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 (rat):289 nM (IC50), TRPA1 receptor (human):67 nM (IC50) |
体内活性 | 系统性注射A 967079(30 micromol/kg)降低了无损伤及CFA炎症大鼠在接受同侧后腿有害钳制刺激后的广动态范围(WDR)和伤害特异性(NS)神经元反应。同样,A-967079也减弱了OA及OA-sham大鼠在接受高强度机械刺激(300 g von Frey hair)对膝关节的WDR神经元反应。此外,A-967079还降低了CFA炎症大鼠在低强度机械刺激(10 g von Frey hair)下的WDR神经元反应,但在未受伤大鼠中无明显效果。A-967079注射后CFA炎症大鼠的WDR神经元自发活动也有所减少,但在未受伤、OA及OA-sham动物中未见变化[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 |
Smiles | CC\C(=N/O)\C(\C)=C\c1ccc(F)cc1 |
密度 | 1.03 g/cm3 at 20℃ |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (482.53 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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