1. Neuronal Signaling Autophagy Apoptosis
  2. Serotonin Transporter Autophagy Apoptosis
  3. Imipramine

Imipramine  (Synonyms: 米帕明)

目录号: HY-B1490A 纯度: 99.88%
COA 产品使用指南 技术支持

Imipramine 是一种具有口服活性的叔胺类三环抗抑郁药。Imipramine 是一种具有抗肿瘤活性的 Fascin1 抑制剂。Imipramine 也抑制 5-羟色胺转运体 (serotonin transporter),其 IC50 值为 32 nM。Imipramine 刺激 U-87MG 胶质瘤细胞自噬(autophagy),诱导 HL-60 细胞凋亡(apoptosis)。Imipramine 具有神经保护和免疫调节作用。

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Imipramine Chemical Structure

Imipramine Chemical Structure

CAS No. : 50-49-7

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10 mM * 1 mL in DMSO ¥715
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Other Forms of Imipramine:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5].

IC50 & Target

Fascin1, Serotonin Transporter, Autophagy, Apoptosis[1][2][3][5]
IC50: 32 nM (human placental serotonin transporter)[5]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
5.1 nM
Compound: Imipramine
Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method
Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method
[PMID: 27865645]
CHO IC50
8.8 x 10-10 M
Compound: Imipramine
Displacement of [3H]imipramine from human recombinant 5HT transporter expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]imipramine from human recombinant 5HT transporter expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
DG-75 IC50
> 50 μM
Compound: Imipramine
Reduction in cell viability of human DG75 cells after 24 hrs by Alamar blue viability assay
Reduction in cell viability of human DG75 cells after 24 hrs by Alamar blue viability assay
[PMID: 23385211]
HEK293 IC50
17.1 μM
Compound: Imipramine
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
HEK293 IC50
2.6 nM
Compound: 1
Inhibition of human SERT W103A mutant expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter
Inhibition of human SERT W103A mutant expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter
[PMID: 27160055]
HEK293 IC50
7.95 μM
Compound: Imipramine
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
[PMID: 28230985]
HeLa IC50
40.74 μM
Compound: Imipramine
Reduction in cell viability of human HeLa cells after 24 hrs by Alamar blue viability assay
Reduction in cell viability of human HeLa cells after 24 hrs by Alamar blue viability assay
[PMID: 23385211]
Ventricular myocyte IC50
4.05 μM
Compound: Imipramine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
8.3 μM
Compound: Imipramine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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: DLD-1, HCT-116, and SW-480
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.

Apoptosis Analysis[3]

Cell Line: HL-60
Concentration: 80 μM
Incubation Time: 24 h
Result: Induced cell apoptosis.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
分子量

280.41

Formula

C19H24N2

CAS 号
性状

粘稠液体

颜色

Colorless to light yellow

中文名称

米帕明

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 200 mg/mL (713.24 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5662 mL 17.8310 mL 35.6621 mL
5 mM 0.7132 mL 3.5662 mL 7.1324 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (17.83 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (17.83 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.88%

参考文献

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5662 mL 17.8310 mL 35.6621 mL 89.1552 mL
5 mM 0.7132 mL 3.5662 mL 7.1324 mL 17.8310 mL
10 mM 0.3566 mL 1.7831 mL 3.5662 mL 8.9155 mL
15 mM 0.2377 mL 1.1887 mL 2.3775 mL 5.9437 mL
20 mM 0.1783 mL 0.8916 mL 1.7831 mL 4.4578 mL
25 mM 0.1426 mL 0.7132 mL 1.4265 mL 3.5662 mL
30 mM 0.1189 mL 0.5944 mL 1.1887 mL 2.9718 mL
40 mM 0.0892 mL 0.4458 mL 0.8916 mL 2.2289 mL
50 mM 0.0713 mL 0.3566 mL 0.7132 mL 1.7831 mL
60 mM 0.0594 mL 0.2972 mL 0.5944 mL 1.4859 mL
80 mM 0.0446 mL 0.2229 mL 0.4458 mL 1.1144 mL
100 mM 0.0357 mL 0.1783 mL 0.3566 mL 0.8916 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Imipramine
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HY-B1490A
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