TMU4142

Cat. No.: HY-179579: Data Sheet Handling Instructions
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TMU4142 is a selective 5-HT_1a 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-HT_1a R autoreceptors or serotonergic neuron firing. TMU4142 demonstrates fast-acting efficacy in mouse models of depression. TMU4142 can be used for antidepressants research.

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

TMU4142 Chemical Structure

Size	Price	Stock
5 mg		Ask For Quote & Lead Time
10 mg		Ask For Quote & Lead Time
25 mg		Ask For Quote & Lead Time
50 mg		Ask For Quote & Lead Time

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

5-HT_1A 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-HT_1a receptor, demonstrates a higher potency at the 5-HT_1a 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

TMU414 (0.3 or 1.5 mg/kg, i.p.) has GoA-biased with minimal Gi3 activity, selectively activates the GoA signaling pathway (primarily localized postsynaptically and antidepressant responses) while avoiding the Gi3-mediated feedback of presynaptic autoreceptors, preserves 5-HT synthesis and release in the DRN in chronic restraint stress-induced depression model in C57BL/6 mice^[1].

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

Animal Model:	Chronic restraint stress (CRS)-induced depression model in male C57BL/6Jmice (8-12 weeks)^[1]
Dosage:	0.3 or 1.5 mg/kg
Administration:	i.p., once
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-HT_1a 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-HT_RA. 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-HT_1a Ractivation. Did not alter DRN5-HT levels in CRS mice.

Molecular Weight

413.51

Formula

C₂₃H₃₁N₃O₄

SMILES

O[C@@H](CNCCCN1C(CC2(CCCC2)CC1=O)=O)COC3=CC=CC4=C3C=CN4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4183 mL	12.0916 mL	24.1832 mL
5 mM	0.4837 mL	2.4183 mL	4.8366 mL
10 mM	0.2418 mL	1.2092 mL	2.4183 mL

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Handling Instructions (2659 KB)

References

[1]. Wang C, et al. Pathway-selective 5-HT1AR agonist as a rapid antidepressant strategy. Cell. 2025 Dec 11;188(25):7222-7237.e24. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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

TMU4142 Related Classifications

Neurological Disease

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:

TMU4142TMU 4142TMU-41425-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT_{1_a}GoAantidepressantDRN 5-HT1ARautoreceptorsInhibitorinhibitorinhibit

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