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Trazodone

Name: Trazodone
Brand: TargetMol
SKU: T22442
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T22442Cas No. 19794-93-5

Alias AF-1161

Trazodone (AF-1161), a 5-HT 2A/2C receptor antagonist, is used as an antidepressant for treating major anxiety disorders and depressive disorder.

Trazodone

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Purity: 99.92%

Catalog No. T22442Alias AF-1161Cas No. 19794-93-5

Trazodone (AF-1161), a 5-HT 2A/2C receptor antagonist, is used as an antidepressant for treating major anxiety disorders and depressive disorder.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$40	In Stock	In Stock
50 mg	$66	In Stock	In Stock
100 mg	$107	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$44	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.92%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Trazodone AI Summary

Trazodone exhibits a range of bioactivities and pharmacokinetic properties, signifying its potential multi-target therapeutic effects. It possesses a low unbound fraction in plasma (Fu = 0.07) and tissues (Fu = 0.03), indicative of high protein binding. Its volume of distribution in humans is moderate (Vdss = 1.0 L.kg-1), indicating it distributes into tissues effectively. The compound has a slightly basic dissociation constant with a pKa value between 6.7 and 6.79 and a moderate lipophilicity evidenced by log D values ranging from 2.54 to 2.99 at pH 7.4. Pharmacologically, Trazodone shows moderate potency in displacing [3H]prazosin from the Alpha-1 adrenergic receptor in the rat cerebral cortex with an IC50 value of 281.0 nM. It also inhibits Batrachotoxinin binding to voltage-dependent sodium channels, displaying an inhibition of 26.2% at 10 uM and 79.6% at 100 uM. Its bioactivity extends to various receptors including significant inhibition of 5-HT2A, alpha-1 adrenergic, and sigma opioid receptors, moderate inhibition of serotonin and dopamine receptors, and negligible inhibition of norepinephrine and histamine receptors. Additionally, it shows a binding constant (Ki) of 223.87 nM to the rat brain 5-HT1A receptor and demonstrates bioactivity against serotonin, adrenergic, dopamine, histamine, and opioid receptors. Trazodone exhibits significant pharmacokinetic and pharmacodynamic characteristics, including oral bioavailability of over 80%, a half-life of approximately 7.3 hours when administered intravenously, and a hepatic clearance of 1.4 mL/min/kg. It demonstrates varying degrees of enzyme inhibition and transporter interactions, such as weak inhibition of human BSEP, MRP3, and MRP4 transporters. Moreover, this compound has demonstrated inhibition in several enzymatic assays, including an IC50 greater than 20000.0 nM against SARS-CoV-2 cytotoxicity in VERO-6 cells. Its wide array of bioactivities covers inhibition of human FAAH, antagonism of drug-induced liver injury, and hepatotoxicity, suggesting extensive therapeutic or toxicological potential. Additionally, Trazodone interacts significantly with various signaling pathways, indicative of multi-faceted pharmacological effects..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Trazodone (AF-1161), a 5-HT 2A/2C receptor antagonist, is used as an antidepressant for treating major anxiety disorders and depressive disorder.
Synonyms	AF-1161

Chemical Properties

Molecular Weight	371.86
Formula	C₁₉H₂₂ClN₅O
Cas No.	19794-93-5
Smiles	O=C1N2C(=NN1CCCN3CCN(CC3)C4=CC(Cl)=CC=C4)C=CC=C2
Relative Density.	1.33g/cm3

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 15 mg/mL (40.34 mM), Sonication is recommended.

H2O: Insoluble

DMSO: 83.33 mg/mL (224.09 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.38 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6892 mL	13.4459 mL	26.8918 mL	134.4592 mL
5 mM	0.5378 mL	2.6892 mL	5.3784 mL	26.8918 mL
10 mM	0.2689 mL	1.3446 mL	2.6892 mL	13.4459 mL
20 mM	0.1345 mL	0.6723 mL	1.3446 mL	6.7230 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0538 mL	0.2689 mL	0.5378 mL	2.6892 mL
100 mM	0.0269 mL	0.1345 mL	0.2689 mL	1.3446 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc