1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. 5-HT Receptor Serotonin Transporter Histamine Receptor Adrenergic Receptor
  3. Trazodone hydrochloride

トラゾドン塩酸塩  (Synonyms: Trazodone (hydrochloride); AF-1161)

製品番号: HY-B0478 純度: 99.60%
COA 取扱説明書 Technical Support

Trazodone hydrochloride (AF-1161) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone hydrochloride has anti-depressant and anti-insomnious activity. Trazodone hydrochloride exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects.

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Trazodone hydrochloride

トラゾドン塩酸塩 構造式

CAS 番号 : 25332-39-2

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 27 在庫あり
Solution
10 mM * 1 mL in DMSO USD 27 在庫あり
Solid
100 mg $25 在庫あり
500 mg $50 在庫あり
1 g $70 在庫あり
5 g $167 在庫あり
10 g $250 在庫あり
50 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 6 publication(s) in Google Scholar

Other Forms of Trazodone hydrochloride:

Top Publications Citing Use of Products
  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Trazodone hydrochloride (AF-1161) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone hydrochloride has anti-depressant and anti-insomnious activity. Trazodone hydrochloride exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects[1].

IC50 & Target

5-HT Receptor[1].

体外実験

Trazodone binds to 5-HT1A receptor with a Ki of 23.6 nM[3].
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[5]

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

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.
体内実験

Trazodone (1.5 mg/kg, i.p., single dose) reduces spontaneous motor activity in cats and dogs[2].
Trazodone (100 mg/kg, i.p., single dose) reduces hyperactivity, prostration and clonic convulsions in cats and dogs[2].
Trazodone (12.5-25 mg/kg, i.p., single dose) inhibits nicotine- and Oxotremorine (HY-170032)-induced tremor[2].
Trazodone (5-20 mg/kg/day, s.c., 2-14 d) significantly decreases the spontaneous firing rate of DR 5-HT neurons by 40% and 37% with 10 and 20 mg/kg dose in SD rats[4].

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

Animal Model: Male Sprague-Dawley rats (250-350 g)[4]
Dosage: 5, 10, 20 mg/kg/day
Administration: 5, 10, 20 mg/kg/day
Result: Induced a marked physiological action on 5-HT neurons.
Significantly decreased the spontaneous firing rate of DR 5-HT neurons by 40% and 37% with 10 and 20 mg/kg dose, respectively.
Blocked 5-HT reuptake process.
分子量

408.32

分子式

C19H23Cl2N5O

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)N=C4C=CC=CN41.Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

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

溶剤 & 溶解度
体外: 

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
10 mM 0.2449 mL 1.2245 mL 2.4491 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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).
純度とドキュメンテーション
参考文献

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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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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.

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Inquiry Information

製品名:
Trazodone hydrochloride
製品番号:
HY-B0478
数量:
MCE 日本正規代理店: