HC-070
目录号 : GC30799
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9.3nM和46nM。
Cas No.:1628291-95-1
Sample solution is provided at 25 µL, 10mM.
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HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.
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 La3+- 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 neuronal activity in the amygdala slices[1].
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[1].
[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.
Animal experiment: | Mice[1]The room is illuminated with fluorescent lighting on a 12-hour light/dark cycle. The light cycle is reversed, so that the dark cycle is from 6 am-6 pm daily and studies are performed when animals are more active. Groups of male C57/BL6 mice (10 weeks old) are dosed PO with 0.5% methyl cellulose or HC-070 at 0.3, 1 or 3 mg/kg (n = 10). The positive control, 1.5 mg/kg diazepam, is administered IP 30 minutes prior to testing (n = 10). Immediately following dosing, mice are returned to their home cage. At 60 minutes post vehicle or HC-070 administration, and 30 minutes post diazepam administration, mice are placed onto the elevated plus maze, one at a time, and their session recorded for 5 minutes. Videos are manually scored for number of open arm entries by a scorer blinded to treatment. All animals that fall off the maze during the test are removed from analysis[1]. |
References: [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. | |
| Cas No. | 1628291-95-1 | SDF | |
| Canonical SMILES | O=C(N1CCCO)N(C)C2=C(N(CC3=CC=C(Cl)C=C3)C(OC4=CC=CC(Cl)=C4)=N2)C1=O | ||
| 分子式 | C22H20Cl2N4O4 | 分子量 | 475.32 |
| 溶解度 | DMSO : ≥ 62.5 mg/mL (131.49 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1038 mL | 10.5192 mL | 21.0385 mL |
| 5 mM | 0.4208 mL | 2.1038 mL | 4.2077 mL |
| 10 mM | 0.2104 mL | 1.0519 mL | 2.1038 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet