HC-070
目录号: PL12455 纯度: ≥99%
CAS No. :1628291-95-1
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中文名称
HC-070
中文别名
化合物 T15465
英文名称
HC-070
英文别名
HC-070;HC-070 (HC070);1H-Purine-2,6-dione, 8-(3-chlorophenoxy)-7-[(4-chlorophenyl)methyl]-3,7-dihydro-1-(3-hydroxypropyl)-3-methyl-
Cas No.
1628291-95-1
分子式
C22H20Cl2N4O4
分子量
475.32
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
HC-070 是一种瞬时受体电位通道蛋白 4/5 (TRPC4/TRPC5) 拮抗剂,在细胞中,对 hTRPC5 和 hTRPC4 的 IC50 值分别为 9.3 nM 和 46 nM。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
IC50: 9.3 nM (hTRPC5, cell assay), 46 nM (hTRPC4, cell assay)
体外研究(In Vitro)
HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4, respectively. HC-070 weakly inhibits TRPC3 (IC50, 1 μM), and is at least 400-fold selective for human TRPC4 and TRPC5-containing channels versus the other channels examined. HC-070 inhibits lanthanum-activated hTRPC5-, mTRPC5-, rTRPC5-mediated currents with IC50s of 0.52 nM, 0.55 nM, and 0.32 nM in whole-cell manual patch clamp. Furthermore, HC-070 blocks M2R-activated human TRPC1/TRPC4 channels with an IC50 of 1.3 nM and La- and M1R-activated human TRPC1/5 channels with IC50s of 1.4 nM and 4.4 nM. HC-070 inhibits human TRPC5 currents activated via muscarinic type 1 (M1R) with an IC50 of 2.0 nM. HC-070 also suppresses hTRPC4 currents via M2R with an IC50 of 0.49 nM. HC-070 (20 nM) reduces CCK-4 evoked neurona
体内研究(In Vivo)
HC-070 (1 mg/kg, p.o.) affects mice with increased evoked anxiety (CCK-4), but shows no effects in the absence of CCK-4. HC-070 (0.3, 1 or 3 mg/kg, p.o.) decreases anxiety in a standard EPM (more light/high anxiety). HC-070 (1 mg/kg) reduces the increased capacity for fear memory in mice subjected to chronic social stress on days 1-15. In addition, HC-070 (1, 3, 10 mg/kg, p.o.) causes reduction in marble burying behavior. HC-070 (0.3, 1, 3, 10 mg/kg, p.o.) also reduces time of immobility in a tail suspension test but does not impact locomotor activity in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Just S, et al. Treatment with HC-070, a potent inhibitor of TRPC4 and TRPC5, leads to anxiolytic and antidepressant effects in mice. PLoS One. 2018 Jan 31;13(1):e0191225.
溶解度数据
In Vitro: DMSO : ≥ 62.5 mg/mL (131.49 mM)配制储备液
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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