Imipramine hydrochloride 是一种具有口服活性的叔胺类三环抗抑郁药。Imipramine hydrochloride 是一种具有抗肿瘤活性的Fascin1抑制剂。Imipramine hydrochloride 也抑制 5-羟色胺转运体 (serotonin transporter)，其IC50值为 32 nM。Imipramine hydrochloride 刺激 U-87MG 胶质瘤细胞自噬（autophagy），诱导 HL-60 细胞凋亡（apoptosis）。Imipramine hydrochloride 具有神经保护和免疫调节作用。
| 生物活性 | Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is aFascin1inhibitor with antitumor activities. Imipramine hydrochloride also inhibitsserotonin transporterwith anIC50value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cellsautophagyand induces HL-60 cellapoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects[1][2][3][4][5]. |
| IC50& Target | Fascin1, Serotonin Autophagy, Apoptosis[1][2][3][5]
IC50: 32 nM (human placental serotonin transporter)[5] |
体外研究
(In Vitro) | Imipramine (0.5-300 μM, 3 days) inhibits HCT-116 cell viability[1].
Imipramine (20 μM) inhibits cell migration (7 h) and invasion (48 h)[1].
Imipramine (50 μM, 0-240 min) inhibites the PI3K/Akt/mTOR signaling pathway in U-87MG glioma cells[2].
Imipramine (60 μM, 24 h) stimulates U-87MG glioma cells autophagy[2].
Imipramine (80 μM, 24 h) induces HL-60 cell apoptosis[3].
Cell Viability Assay[1] | Cell Line: | DLD-1, HCT-116, and SW-480 | | Concentration: | 0.5-300 μM | | Incubation Time: | 3 days | | Result: | Inhibited cell viability and HCT-116 was more sensitive than DLD-1 and SW-480. |
Cell Migration Assay[1] | Cell Line: | SW-480, DLD-1, and HCT-116 | | Concentration: | 20 μM | | Incubation Time: | 7 h | | Result: | Produced a remarkable inhibition of migration in all assayed cell lines. |
Cell Invasion Assay[1] | Cell Line: | HCT-116 | | Concentration: | 20 μM | | Incubation Time: | 48 h | | Result: | Inhibited cell invasion through Matrigel. |
Western Blot Analysis[2] | Cell Line: | U-87MG | | Concentration: | 50 μM | | Incubation Time: | 0, 15, 30, 60, 120 and 240 min | | Result: | Markedly inhibited the phosphorylation of both Akt (Ser473) and mTOR (Ser2481) in a time-dependent manner. Also dephosphorylated p70 S6K, a downstream target of mTOR. |
Cell Autophagy Assay[2] | Cell Line: | U-87MG | | Concentration: | 60 μM | | Incubation Time: | 24 h | | Result: | Stimulated the induction of autophagy through the redistribution of LC3 in U-87MG glioma cells. |
Cell Autophagy Assay[3] | Cell Line: | HL-60 | | Concentration: | 80 μM | | Incubation Time: | 24 h | | Result: | Induced cell apoptosis. |
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体内研究
(In Vivo) | Imipramine (20 mg/kg, i.p. or 15 mg/kg, p.o.; daily for 24 days) attenuates neuroinflammatory signaling and reverses stress-induced social avoidance in mice[4].
| Animal Model: | Male C57BL/6 mice (6–8 weeks old) subjected to RSD (repeated social defeat) and HCC (home cage control)[4] | | Dosage: | 20 mg/kg or 15 mg/kg | | Administration: | Intraperitoneal injection or oral administration, daily for 24 days | | Result: | Reversed RSD-induced social avoidance behavior, significantly increasing the interaction time, significantly decreased stress-induced mRNA levels for IL-6 in brain microglia. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(315.59 mM) H2O : 62.5 mg/mL(197.24 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.1559 mL | 15.7793 mL | 31.5587 mL | | 5 mM | 0.6312 mL | 3.1559 mL | 6.3117 mL | | 10 mM | 0.3156 mL | 1.5779 mL | 3.1559 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 60 mg/mL (189.35 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.89 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.89 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.89 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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