MAO-A/5-HT2AR-IN-1
Based on 1 Customer Validation
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.
- Purity: 99.71%
- CAS No.: 2769156-00-3
- Formula: C30H28FN3O2
- Molecular Weight:481.56
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
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MAO-A 0.004 ± 0. μM (IC50) |
5-HT2A Receptor 0.014 μM (IC50) |
MAO-B 1.05 ± 0.0 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| L02 | IC50 |
>100 μM
Compound: Cpd I9
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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
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[PMID: 36173886] |
| PC-12 | IC50 |
>10 μM
Compound: Cpd I9
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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
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[PMID: 36173886] |
| SH-SY5Y | IC50 |
>10 μM
Compound: Cpd I9
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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
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[PMID: 36173886] |
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 (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.
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Animal Model:ICR male mice (8−10 weeks old, weight 18-20 g)[1]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:For 2 weeks
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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.
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Animal Model:Zebrafish (AB strain, Reserpine-induced zebrafish depression model)[1]
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Dosage:0.1, 0.5, 1 μM
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Administration:Given 24 h after reserpine, for 7 days.
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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.
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Animal Model:Sprague-Dawley rats (male)[1]
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Dosage:2 mg/kg (i.v.) 10 mg/kg (i.g.)
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Administration:IV, IG; once (Pharmacokinetic Analysis)
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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
Chemical Information
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CAS No. 2769156-00-3
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Appearance Solid
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Molecular Weight 481.56
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Formula C30H28FN3O2
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Color Light yellow to yellow
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SMILES
O=C1C2=C(C3=NC=CC4=CC(OCCCCN5CCN(CC5)C6=C(F)C=CC=C6)=CC1=C43)C=CC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMF : 1 mg/mL (2.08 mM; ultrasonic and warming and heat to 60°C)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: 10% DMF 90% Corn Oil
Solubility: 0.5 mg/mL (1.04 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 |
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| DMF | 1 mM | 2.0766 mL | 10.3829 mL | 20.7658 mL | 51.9146 mL |
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