2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Trazodone hydrochloride

Trazodone hydrochloride  (Synonyms: AF-1161)

Cat. No.: HY-B0478 Purity: 99.61%
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Trazodone hydrochloride (AF-1161) is a serotonin receptor antagonist and reuptake inhibitor with anti-neuroinflammatory effects. Trazodone hydrochloride can be used for research in major depressive disorder and also holds potential for studies related to sleep disorders.

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

Trazodone hydrochloride Chemical Structure

Trazodone hydrochloride Chemical Structure

CAS No. : 25332-39-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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500 mg In-stock
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Based on 2 publication(s) in Google Scholar

Other Forms of Trazodone hydrochloride:

Trazodone hydrochloride Related Antibodies

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Description

Trazodone hydrochloride (AF-1161) is a serotonin receptor antagonist and reuptake inhibitor with anti-neuroinflammatory effects. Trazodone hydrochloride can be used for research in major depressive disorder and also holds potential for studies related to sleep disorders[1][2][3][4].

IC50 & Target

5-HT Receptor[1].
In Vitro

Trazodone (1 nM–10 μM, 24 h or 72 h) reduces the expression of neuroinflammatory markers by inhibiting key signaling pathways such as NF-κB, p38 MAPK, and JNK, exhibiting neuroprotective effects[4].

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

Trazodone hydrochloride Related Antibodies

Real Time qPCR[4]

Cell Line: Neuronal-like cells differentiated from H9-derived NSCs
Concentration: 1 nM–10 μM
Incubation Time: 24 h or 72 h
Result: Increased mRNA expression of BDNF and CREB, reduced IFN-γ release.

Western Blot Analysis[4]

Cell Line: Neuronal-like cells differentiated from H9-derived NSCs
Concentration: 1 nM–10 μM
Incubation Time: 24 h or 72 h
Result: Showed increased levels of phosphorylated ERK1/2 and decreased phosphorylated p38 levels.

Cell Proliferation Assay[4]

Cell Line: Neuronal-like cells differentiated from H9-derived NSCs
Concentration: 1 nM–10 μM
Incubation Time: 24 h or 72 h
Result: Didn't show significant effects on cell proliferation or viability at tested concentrations.
In Vivo

Trazodone (40 mg/kg, i.p., once daily for 9 weeks) reduces key cellular components of neuroinflammation and related protein expression in the tauopathy rTg4510 mouse model, exhibiting anti-neuroinflammatory effects[2].
Trazodone was administered intravenously (8 mg/kg) and orally (8.26 mg/kg) to dogs in a pharmacokinetic study, demonstrating high bioavailability, moderate plasma concentration, and stable elimination half-life in dogs. After oral administration, Trazodone had an average absolute bioavailability of 84.6%, with an elimination half-life of T1/2 = 166 minutes. The maximum plasma concentration (Cmax) after oral administration was 1.3 μg/mL, and the time to reach maximum plasma concentration (Tmax) was 445 minutes. The elimination half-life after intravenous administration was T1/2 = 169 minutes[3].

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

Animal Model: Tauopathy rTg4510 mouse model ( Expression of the P301L tau mutant protein driven by the tetracycline-responsive element in male rTg4510 mice with a FVB/NCrl1 × 129S6/SvEvTa background and an average body weight of 29.3 g)[2]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily, for 9 weeks
Result: Significantly reduced microglial activation and NLRP3 inflammasome expression. Decreased phosphorylated p38 MAPK and ATF4 protein levels in the cortex.
Clinical Trial
Molecular Weight

408.32

Formula

C19H23Cl2N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)N=C4C=CC=CN41.Cl
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 : 16.67 mg/mL (40.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 16.67 mg/mL (40.83 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4491 mL 12.2453 mL 24.4906 mL
5 mM 0.4898 mL 2.4491 mL 4.8981 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.

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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: ≥ 1.67 mg/mL (4.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (4.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
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 (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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.4491 mL 12.2453 mL 24.4906 mL 61.2265 mL
5 mM 0.4898 mL 2.4491 mL 4.8981 mL 12.2453 mL
10 mM 0.2449 mL 1.2245 mL 2.4491 mL 6.1226 mL
15 mM 0.1633 mL 0.8164 mL 1.6327 mL 4.0818 mL
20 mM 0.1225 mL 0.6123 mL 1.2245 mL 3.0613 mL
25 mM 0.0980 mL 0.4898 mL 0.9796 mL 2.4491 mL
30 mM 0.0816 mL 0.4082 mL 0.8164 mL 2.0409 mL
40 mM 0.0612 mL 0.3061 mL 0.6123 mL 1.5307 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.

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Trazodone hydrochloride Related Classifications

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:

Trazodone25332-39-2AF-1161AF1161AF 11615-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorNeuronal-like cellsNeuroprotective effectsTauopathy rTg4510 mouse modelInhibitorinhibitorinhibit

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