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Trazodone

Name: Trazodone
Brand: TargetMol
SKU: T22442
Price: 193 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.92%

货号 T22442Cas号 19794-93-5

别名 曲唑酮, AF-1161

Trazodone (AF-1161) 是一种 5-HT 2A/2C 受体拮抗剂，用作治疗主要焦虑症和抑郁症的抗抑郁药。

Trazodone

一键复制产品信息

很棒

纯度: 99.92%

货号 T22442 别名 曲唑酮, AF-1161Cas号 19794-93-5

Trazodone (AF-1161) 是一种 5-HT 2A/2C 受体拮抗剂，用作治疗主要焦虑症和抑郁症的抗抑郁药。

规格	价格	库存
10 mg	¥ 208	现货
25 mg	¥ 329	现货
50 mg	¥ 475	现货
100 mg	¥ 672	现货
1 mL x 10 mM (in DMSO)	¥ 193	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

常见问题解答

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纯度: 99.92%

颜色: 白色

性状: Solid

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资源下载:

COA HNMR LCMS 产品操作手册

产品介绍

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

生物活性

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

化学信息

分子量	371.86
分子式	C₁₉H₂₂ClN₅O
CAS No.	19794-93-5
Smiles	O=C1N2C(=NN1CCCN3CCN(CC3)C4=CC(Cl)=CC=C4)C=CC=C2
密度	1.33g/cm3

储存&溶解度

存储

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.

溶解度信息

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

H2O: Insoluble

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

体内实验配方

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

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法： 取 100 μL DMSO 母液，添加 400 μL PEG300 混匀澄清，再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH₂O 混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如： DMSO， PEG300， PEG400， Tween 80， SBE-β-CD，玉米油等，均可在TargetMol网站点击购买。

剂量转换

对于不同动物的给药剂量换算，您也可以参考更多

关键词

Trazodone serotonin reuptake AF1161 AF 1161 5HTReceptor 5HT Receptor

Trazodone

Trazodone

Trazodone 相关产品

产品介绍

计算器

体内实验配液计算器

剂量转换

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