Trimipramine maleate

Name: Trimipramine maleate
Brand: MedChemExpress
SKU: HY-B1213
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1213 Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Trimipramine maleate is a 5-HT receptor antagonist, with pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC₅₀ values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy.

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

Trimipramine maleate Chemical Structure

CAS No. : 521-78-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Trimipramine maleate:

Trimipramine-d₃ maleate Get quote
Trimipramine Get quote
Trimipramine maleate (Standard) Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Trimipramine maleate is a 5-HT receptor antagonist, with pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, respectively^[1]. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC₅₀ values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively^[2]. Trimipramine maleate has vascular activity and anxiolytic efficacy^[3].

IC₅₀ & Target

5-HT_1C Receptor

6.39 (pKi)

5-HT₂ Receptor

8.10 (pKi)

sPLA2

4.66 (pKi)

In Vitro

Trimipramine maleate displays much higher affinity for 5-HT₂ than for 5-HT_1C receptors^[1].
Trimipramine maleate is a moderate inhibitor of the human NAT and SERT, with the IC₅₀ values of 4.99 μM and 2.11 μM, respectively^[2].
SERT and NAT could represent a target for the antidepressant effects of trimipramine maleate (1 mM, 0.1 mM, 0.01 mM, 1 μM, 0.1 μM; 10 min; HEK293 cells)^[2].

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

In Vivo

Trimipramine maleate (5 mg/kg/d; 14 d; chronic administration) acts as functions in rats:1. Increasing concentration of regional 5-HT. 5-HT is highest in the frontal cortex and the hippocampus, followed by the olfactory tubercles and the hypothalamus. 2. Decreasing the number of frontal cortex 5-HT₂ and striatal DA D₂ receptors. 3. Increasing in the brain regional level of monoamines and metabolites. thus indicates a greater synthesis rate for dopamine (DA) and 5-HT coinciding with an adaptive down regulation of 5-HT₂ and DA D₂ receptors^[3].

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

Animal Model:	Male Wistar rats (220-250 g); implanted osmotic minipump subcutaneously in the dorsal thoracic interscapular region^[3]
Dosage:	5 mg/kg/day
Administration:	Delivered by smotic minipump; 14 days
Result:	Decreased the number of frontal cortex 5-HT₂ and striatal DA D₂ receptors, thus blocked the uptake of 5-HT and dopamine (DA).

Clinical Trial

Molecular Weight

410.51

Formula

C₂₄H₃₀N₂O₄

CAS No.

521-78-8

Appearance

Solid

Color

White to off-white

SMILES

CC(CN(C)C)CN1C2=C(C=CC=C2)CCC3=C1C=CC=C3.O=C(O)/C=C\C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (243.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 14.29 mg/mL (34.81 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4360 mL	12.1800 mL	24.3599 mL
5 mM	0.4872 mL	2.4360 mL	4.8720 mL
10 mM	0.2436 mL	1.2180 mL	2.4360 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 (6.09 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 (6.09 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 (6.09 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 5.88 mg/mL (14.32 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: 99.82%

Select Batch:

Data Sheet (282 KB) SDS (419 KB)

COA (259 KB) RP-HPLC (251 KB)

Handling Instructions (2659 KB)

References

[1]. Jenck F, et al. Evidence for a role of 5-HT1C receptors in the antiserotonergic properties of some antidepressant drugs. Eur J Pharmacol. 1993 Feb 9;231(2):223-9. [Content Brief]

[2]. Haenisch B, et al. Inhibitory potencies of trimipramine and its main metabolites at human monoamine and organic cation transporters. Psychopharmacology (Berl). 2011 Sep. 217(2):289-95. [Content Brief]

[3]. Juorio AV, et al. The effects of chronic trimipramine treatment on biogenic amine metabolism and on dopamine D2, 5-HT2 and tryptamine binding sites in rat brain. Gen Pharmacol. 1990;21(5):759-62. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.4360 mL	12.1800 mL	24.3599 mL	60.8999 mL
	5 mM	0.4872 mL	2.4360 mL	4.8720 mL	12.1800 mL
	10 mM	0.2436 mL	1.2180 mL	2.4360 mL	6.0900 mL
	15 mM	0.1624 mL	0.8120 mL	1.6240 mL	4.0600 mL
	20 mM	0.1218 mL	0.6090 mL	1.2180 mL	3.0450 mL
	25 mM	0.0974 mL	0.4872 mL	0.9744 mL	2.4360 mL
	30 mM	0.0812 mL	0.4060 mL	0.8120 mL	2.0300 mL
DMSO	40 mM	0.0609 mL	0.3045 mL	0.6090 mL	1.5225 mL
	50 mM	0.0487 mL	0.2436 mL	0.4872 mL	1.2180 mL
	60 mM	0.0406 mL	0.2030 mL	0.4060 mL	1.0150 mL
	80 mM	0.0304 mL	0.1522 mL	0.3045 mL	0.7612 mL
	100 mM	0.0244 mL	0.1218 mL	0.2436 mL	0.6090 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.