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) 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.

For research use only. We do not sell to patients.

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

Based on 1 publication(s) in Google Scholar

MAO-A/5-HT2AR-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Monoamine Oxidase Isoform Specific Products:

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MAO-A MAO-B

View All 5-HT Receptor Isoform Specific Products:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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].

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

MAO-A/5-HT2AR-IN-1 Related Antibodies

[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.
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].

MedChemExpress (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
Molecular Weight

481.56

Formula

C30H28FN3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(C3=NC=CC4=CC(OCCCCN5CCN(CC5)C6=C(F)C=CC=C6)=CC1=C43)C=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (41.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 5 mg/mL (10.38 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (4.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (4.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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MAO-A/5-HT2AR-IN-1 Related Classifications

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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