TMU4142
Based on 1 Customer Validation
TMU4142 is a selective 5-HT1a agonist with high GoA activity. TMU4142 has weak Gi3 activity, can elicit rapid antidepressant like effects without triggering significant activation of dorsal raphe nucleus (DRN) 5-HT1a R autoreceptors or serotonergic neuron firing. TMU4142 demonstrates fast-acting efficacy in mouse models of depression. TMU4142 can be used for antidepressants research.
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- Pureté : 98.93%
- Formule: C23H31N3O4
- Masse moléculaire:413.51
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Voir tous les produits spécifiques à Isoform 5-HT Receptor
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Activité biologique
Description
IC50 & Target
[1]|
5-HT1A Receptor |
In Vitro
TMU4142 agonist GoA signaling pathway and weak activity at the Gi3 pathway, shows no discernible activity at the β-arrestin-2 pathway associated with the 5-HT1a receptor, demonstrates a higher potency at the 5-HT1a receptor while reducing activity at β-adrenergic receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chronic restraint stress (CRS)-induced depression model in male C57BL/6Jmice (8-12 weeks)[1]
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Dosage:0.3 or 1.5 mg/kg
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Administration:i.p., once
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Result:Significantly reduced the immobility time of CRS mice in the forced swim test (FST) 30min post-injection indicating an antidepressant-like effect.
Reversed CRS-induced depressive-like behaviors in mice at 1.5mg/kg.
Elicited significant antidepressant-like effects.
Exerted antidepressant-like effects in CRS mice through 5-HT1a R activation, as demonstrated by the blockade of the immobility-reducing effects in the FST and tail suspension test (TST) by the antagonist WAY 100635 (Y-10349).
Abolished the reduction in immobility time in both the FST and TST indicated that the antidepressant-like effects are mediated through the activation of 5-HTRA.
Significantly reduced the latency to feed in mice as early as 1 h after drug administration without affecting the home cage food intake.
Has acute effect in the NSF test was blocked by way-100635, suggesting that its action is mediated through5-HT1a Ractivation.
Did not alter DRN5-HT levels in CRS mice.
Chemical Information
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Appearance Solid
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Masse moléculaire 413.51
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Formule C23H31N3O4
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Color White to off-white
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SMILES
O[C@@H](CNCCCN1C(CC2(CCCC2)CC1=O)=O)COC3=CC=CC4=C3C=CN4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (241.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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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| DMSO | 1 mM | 2.4183 mL | 12.0916 mL | 24.1832 mL | 60.4580 mL |
| 5 mM | 0.4837 mL | 2.4183 mL | 4.8366 mL | 12.0916 mL | |
| 10 mM | 0.2418 mL | 1.2092 mL | 2.4183 mL | 6.0458 mL | |
| 15 mM | 0.1612 mL | 0.8061 mL | 1.6122 mL | 4.0305 mL | |
| 20 mM | 0.1209 mL | 0.6046 mL | 1.2092 mL | 3.0229 mL | |
| 25 mM | 0.0967 mL | 0.4837 mL | 0.9673 mL | 2.4183 mL | |
| 30 mM | 0.0806 mL | 0.4031 mL | 0.8061 mL | 2.0153 mL | |
| 40 mM | 0.0605 mL | 0.3023 mL | 0.6046 mL | 1.5115 mL | |
| 50 mM | 0.0484 mL | 0.2418 mL | 0.4837 mL | 1.2092 mL | |
| 60 mM | 0.0403 mL | 0.2015 mL | 0.4031 mL | 1.0076 mL | |
| 80 mM | 0.0302 mL | 0.1511 mL | 0.3023 mL | 0.7557 mL | |
| 100 mM | 0.0242 mL | 0.1209 mL | 0.2418 mL | 0.6046 mL |
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