A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC 50 of 1.025 μM. A-317567 has antidepressant and antinociception effects.
性状
Solid
IC50 & Target[1][2]
IC50: 1.025 μM (Acid-sensing ion channel 3 (ASIC-3))
体外研究(In Vitro)
在急性分离的成年大鼠背根神经节 (DRG) 神经元中,A-317567 对所有 pH 4.5 诱发的 ASIC 电流产生浓度依赖性抑制,IC50 范围在 2 和 30 μM 之间。A-317567 等效地阻断类 ASIC3 电流的持续相,这是一种类似于克隆 ASIC3 的双相电流,在 DRG 中占主导地位 。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
A-317567 (1-100 μmol/kg; i.p; once) 在 CFA 模型中具有完全镇痛作用 (ED 50 of 17 μmol/kg)。在这些条件下,A-317567 对侧爪子的缩回潜伏期没有显着影响。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Adult male Spra
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Kuduk SD, et al. Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567. ACS Chem Neurosci. 2010 Jan 20;1(1):19-24.[2]. Dubé GR, et al. Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels. Pain. 2005 Sep;117(1-2):88-96.
溶解度数据
In Vitro: DMSO : 50 mg/mL (125.77 mM; ultrasonic and warming and heat to 60°C)配制储备液