2. Neuronal Signaling GPCR/G Protein
  3. Monoamine Oxidase 5-HT Receptor
  4. MAO-A/5-HT2AR-IN-1

MAO-A/5-HT2AR-IN-1 (compound I14) 是一种有效的 MAO-A 和 5-HT2AR 双重抑制剂，其 IC 50 分别为 0.004 和 0.014 μM。MAO-A/5-HT2AR-IN-1 是一种潜在的抗抑郁剂。

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MAO-A/5-HT2AR-IN-1 Chemical Structure

MAO-A/5-HT2AR-IN-1 Chemical Structure

CAS No. : 2769156-00-3

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Customer Review

MAO-A/5-HT2AR-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Monoamine Oxidase 亚型特异性产品:

查看所有亚型
MAO-A MAO-B

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MAO-A/5-HT2AR-IN-1 (compound I14) is a potent MAO-A and 5-HT2AR dual inhibitor, with IC50 values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent[1].

IC50 & Target

MAO-A

0.004 ± 0. μM (IC50)

5-HT2A Receptor

0.014 μM (IC50)

MAO-B

1.05 ± 0.0 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
L02 IC50
> 100 μM
Compound: Cpd I9
Cytotoxicity against human L02 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
[PMID: 36173886]
PC-12 IC50
> 10 μM
Compound: Cpd I9
Cytotoxicity against rat PC-12 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
Cytotoxicity against rat PC-12 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
[PMID: 36173886]
SH-SY5Y IC50
> 10 μM
Compound: Cpd I9
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
[PMID: 36173886]
体外研究
(In Vitro)

MAO-A/5-HT2AR-IN-1 (compound I14) (0-4 μM, 24 h) exhibits a significant neurocytoprotective effect on the CORT-induced cell depression model[1].
MAO-A/5-HT2AR-IN-1 is able to occupy the active cavity of 5-HT2AR and MAO-A with multiple hydrogen bonding forces and π–π stacking interaction[1].
MAO-A/5-HT2AR-IN-1 exhibits low proliferation inhibitory activities against L02 cells (IC50 > 100 μM), SH-SY5Y (IC50 > 10 μM) and PC12 (IC50 > 10 μM), indicating it has a good safety profile[1].

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

MAO-A/5-HT2AR-IN-1 相关抗体:

[1][1]

Cell Line: PC12 cells
Concentration: 4.0, 2.0, 1.0, and 0.5 μM (and 500 μM CORT)
Incubation Time: 24 h
Result: Showed a significant protective effect on PC12 cells injury at different concentrations compared with the model group, where the best protective effect was observed at 0.5 μM.
体内研究
(In Vivo)

MAO-A/5-HT2AR-IN-1 (compound I14) (10 and 20 mg/kg) significantly ameliorates the depression-like behavior of mice[1].
MAO-A/5-HT2AR-IN-1 (0-1 μM, for 7 days) improves zebrafish locomotion and the depression-like behavior[1].
MAO-A/5-HT2AR-IN-1 is able to repair the damage of mice hippocampal neuronal cells and reduce the expression of 5-HT2AR in mice brain tissue[1].
MAO-A/5-HT2AR-IN-1 (2 mg/kg (i.v.) 10 mg/kg (i.g.); once) has a good clearance rate of 345.69 mL/min/kg in rats[1].

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

Animal Model: ICR male mice (8−10 weeks old, weight 18-20 g)[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: For 2 weeks
Result: Significantly improved depression-like behavior in mice, with the low dose group (10 mg/kg) being more potent than with the positive drug (Flu, 20 mg/kg). Had no relevant toxic effects on the liver, kidney, lung, and spleen of mice during the treatment period.
Animal Model: Zebrafish (AB strain, Reserpine-induced zebrafish depression model)[1]
Dosage: 0.1, 0.5, 1 μM
Administration: Given 24 h after reserpine, for 7 days.
Result: Showed that zebrafish in the I14 administered group moved significantly more distance, faster, and spent significantly more time in the upper part compared to the model group.
Animal Model: Sprague-Dawley rats (male)[1]
Dosage: 2 mg/kg (i.v.) 10 mg/kg (i.g.)
Administration: IV, IG; once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of MAO-A/5-HT2AR-IN-1 in male Sprague-Dawley rats[1].
parameter 2 mg/kg (i.v.) 10 mg/kg (i.g.)
Tmax (h) 0.08 ± 0.00 1.33 ± 0.33
Cmax (ng/mL) 673.33 ± 25.41 99.67 ± 6.01
AUC0-24 (ng/mL·h) 2230.67 ± 153.78 490.67 ± 70.43
AUC0-inf (ng/mL·h) 2322.67 ± 178.02 504.00 ± 71.08
t1/2 (h) 6.31 ± 0.55 5.22 ± 0.79
CL (mL/min/kg) 14.54 ± 1.20 345.69 ± 53.40
MRTinf (h) 4.19 ± 0.14 4.94 ± 0.36
F (%) 4.40
分子量

481.56

Formula

C30H28FN3O2
CAS 号
性状

固体

颜色

Light yellow to yellow

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
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 : 20 mg/mL (41.53 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

DMF 中的溶解度 : 5 mg/mL (10.38 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0766 mL 10.3829 mL 20.7658 mL
5 mM 0.4153 mL 2.0766 mL 4.1532 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: ≥ 2 mg/mL (4.15 mM); 澄清溶液

    此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 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: ≥ 2 mg/mL (4.15 mM); 澄清溶液

    此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 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

只
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
参考文献

MAO-A/5-HT2AR-IN-1 相关分类

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
DMF / DMSO 1 mM 2.0766 mL 10.3829 mL 20.7658 mL 51.9146 mL
5 mM 0.4153 mL 2.0766 mL 4.1532 mL 10.3829 mL
10 mM 0.2077 mL 1.0383 mL 2.0766 mL 5.1915 mL
DMSO 15 mM 0.1384 mL 0.6922 mL 1.3844 mL 3.4610 mL
20 mM 0.1038 mL 0.5191 mL 1.0383 mL 2.5957 mL
25 mM 0.0831 mL 0.4153 mL 0.8306 mL 2.0766 mL
30 mM 0.0692 mL 0.3461 mL 0.6922 mL 1.7305 mL
40 mM 0.0519 mL 0.2596 mL 0.5191 mL 1.2979 mL
Help & FAQs
  • 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.

Keywords:

MAO-A/5-HT2AR-IN-12769156-00-3Monoamine Oxidase5-HT ReceptorMAOSerotonin Receptor5-hydroxytryptamine ReceptorneurocytoprotectivePC12 cellsSH-SY5YL02depressionantidepressantInhibitorinhibitorinhibit

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