靶点活性：TRPC5 (human):9.3 nM, TRPC4 (human):46 nM 体外活性： HC-070通过抑制通过毒蕈碱型1激活的hTRPC5电流（IC50 = 2.0 nM）和通过毒蕈碱型2抑制hTRPC4电流（IC50 = 0.49 nM）。在全细胞手动贴片钳技术中，HC-070抑制镧激活的hTRPC5-、mTRPC5-、rTRPC5介导的电流（IC50分别为0.52 nM、0.55 nM和0.32 nM）。在杏仁体切片中，HC-070（20 nM）降低CCK-4诱发的神经元活动。HC-070对TRPC3的抑制作用较弱（IC50 = 1 μM），并阻断M2R激活的人类TRPC1/TRPC4通道（IC50 = 1.3 nM）以及La3+和M1R激活的人类TRPC1/5通道（IC50分别为1.4 nM和4.4 nM）。 体内活性： HC-070 (1 mg/kg) 能够降低因连续社会压力(1-15天)导致的小鼠增强的恐惧记忆能力。HC-070 (1 mg/kg, p.o.) 对于CCK-4引起的焦虑增加的小鼠有影响。HC-070 (0.3-3 mg/kg, p.o.) 在标准EPM测试中减少了焦虑现象。HC-070 (0.3-10 mg/kg, p.o.) 在尾悬挂测试中减少了不动时间，而不影响小鼠的运动活动。HC-070 (1-10 mg/kg, p.o.) 减少了掩埋玻璃珠的行为。 HC-070 is an antagonist of TRPC4/TRPC5 , with IC 50 s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively. Target Activity： TRPC5 (human):9.3 nM, TRPC4 (human):46 nM In vitro Activity ： HC-070 inhibits hTRPC5 currents activated via muscarinic type 1 (IC50 = 2.0 nM) and suppresses hTRPC4 currents via muscarinic type 2 (IC50 = 0.49 nM). In whole-cell manual patch clamp, HC-070 inhibits lanthanum-activated hTRPC5-, mTRPC5-, rTRPC5-mediated currents (IC50s of 0.52 nM, 0.55 nM, and 0.32 nM). In the amygdala slices, HC-070 (20 nM) decreases CCK-4-evoked neuronal activity. HC-070 weakly inhibits TRPC3 (IC50 = 1 μM) and blocks M2R-activated human TRPC1/TRPC4 channels (IC50 = 1.3 nM) and La3+- and M1R-activated human TRPC1/5 channels (IC50 = 1.4 nM and 4.4 nM). In vivo Activity： HC-070 (1 mg/kg) reduces the increased capacity for fear memory in mice subjected to chronic social stress on days 1-15. HC-070 (1 mg/kg, p.o.) affects mice with increased CCK-4-evoked anxiety. HC-070 (0.3-3 mg/kg, p.o.) causes a reduction of anxiety in a standard EPM. HC-070 (0.3-10 mg/kg, p.o.) reduces the time of immobility in a tail suspension test without impacting locomotor activity in mice. HC-070 (1-10 mg/kg, p.o.) reduces marble-burying behavior.
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HC-070
CAS number：1628291-95-1 molecular formula：C22H20Cl2N4O4
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| Chinese alias | 7-(4-氯苄基)-8-(3-氯苯氧基)-1-(3-羟丙基)-3-甲基-3,7-二氢-1H-嘌呤-2,6-二酮 | ||
| English alias | 8-(3-chlorophenoxy)-7-[(4-chlorophenyl)methyl]-1-(3-hydroxypropyl)-3-methylpurine-2,6-dione | 8-(3-chloranylphenoxy)-7-[(4-chlorophenyl)methyl]-3-methyl-1-(3-oxidanylpropyl)purine-2,6-dione | 7-(4-Chlorobenzyl)-8-(3-chlorophenoxy)-1-(3-hydroxypropyl)-3-me | ||
| CAS number | 1628291-95-1 | molecular formula | C22H20Cl2N4O4 |
| molecular weight | 475.32 g/mol | Exact mass | - |
| PSA | 87.900 Ų | logp | 4.000 |
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