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Pizotifen

Name: Pizotifen
Brand: TargetMol
SKU: T1442
Price: 198 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.93%

货号 T1442Cas号 15574-96-6

别名 苯噻啶, Pizotyline, BC-105

Pizotifen (Pizotyline) 是5-HT2受体的有效拮抗剂，并对5-HT1C 有高亲和力。它是一种强血清素和色胺拮抗剂，具有较弱的抗胆碱能、抗组胺和抗激肽作用，还具有镇静和刺激食欲的特性。

Pizotifen

一键复制产品信息

很棒

纯度: 99.93%

货号 T1442 别名 苯噻啶, Pizotyline, BC-105Cas号 15574-96-6

规格	价格	库存
50 mg	¥ 198	现货
100 mg	¥ 356	现货
200 mg	¥ 671	现货
500 mg	¥ 1,174	现货
1 mL x 10 mM (in DMSO)	¥ 460	现货

库存状态实时更新，以官网显示为准，现货产品可直接加购物车下单

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实验操作小课堂

常见问题解答

选择批次:

纯度: 99.93%

颜色: 白色

性状: Solid

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COA HNMR LCMS 产品操作手册

产品介绍

Pizotifen AI Summary

Pizotifen exhibits a diverse range of bioactivities and pharmacological properties. It has been assessed for binding energy, showing a binding energy of 13.0 kCal mol-1 calculated using the equation deltaG obsd = -RT ln KD. This indicates its strong binding affinity to target molecules, providing insights into its potential bioactivities and interactions. In mouse models, Pizotifen demonstrates antagonism towards 5-hydroxytryptophan (5-HTP) when administered subcutaneously in doses ranging from 0.003 to 0.1 mg/kg, with an ED50 of 0.015 mg/kg after 0.5 hours. It has shown significant results in assays including modulation of Lamin A splicing, inhibition of IMPase, and potentiation by Lithium. It also inhibits malarial parasite plastid, Schwann cell viability, human tyrosyl-DNA phosphodiesterase 1, Plasmodium falciparum proliferation, and viral entry for Lassa, Marburg, and Ebola viruses. Notably, it has been identified for its gametocytocidal activity. No hepatic side effects have been detected based on the Drug-Induced Liver Injury Prediction System (DILIps), with all scores reported as 0.0 for various liver conditions, indicating minimal to no liver toxicity. Pizotifen exhibits high binding affinity towards muscarinic M1, dopamine D2, 5-HT2C, and 5-HT2B receptors (Ki values: 1.4 to 2.4 nM) and moderate affinity towards adrenergic alpha1 and 5-HT2A receptors (Ki values: 75.0 nM and 7.5 nM, respectively). It also displaces radiolabeled ligands from human 5-HT7 and 5-HT2B receptors, suggesting potent interactions with multiple neurotransmitter receptors. While it shows moderate cholestatic liver toxicity and low-frequency acute liver toxicity, it has not been predominantly associated with severe hepatic conditions like cytolytic toxicity, hepatitis, cirrhosis, or tumors. Regarding anti-parasitic and cytotoxic activities, Pizotifen has varying IC50 values across different assays, indicating potential utility against malaria, Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis, and cytotoxicity in various cell types. For antiviral activity, it has an IC50 greater than 20,000.0 nM against SARS-CoV-2 in VERO-6 cells, implying a requirement for high concentrations for effective results. Additionally, it inhibits human HDAC6 enzyme activity, with slight inhibitory increase and a particular profile of inhibition when tested with custom versus commercial peptide substrates. Lastly, Pizotifen shows antagonist activity at human HRH1 (AC50 = 68.1 nM) and inhibits human KCNH2 (AC50 = 2307.0 nM), along with various actions at HRH2, ADRB2, HTR2A, HTR1A, ADRA1A, CNR1, and GABRA1 receptors, indicating a broad spectrum of pharmacological effects..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述

Pizotifen (Pizotyline) is a strong serotonin and tryptamine antagonist, with weak anticholinergic, anti-histaminic and anti-kinin effects. It also possesses sedative and appetite-stimulating properties. Pizotifen hydrochloride is an active ingredient in Sandomigran, which is used for the prophylactic management of migraine. Sandomigran is available in number of countries excluding the United States.

别名

苯噻啶, Pizotyline, BC-105

化学信息

分子量	295.44
分子式	C₁₉H₂₁NS
CAS No.	15574-96-6
Smiles	CN1CCC(CC1)=C1c2ccsc2CCc2ccccc12
密度	1.164 g/cm3 (Predicted)

储存&溶解度

存储

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

H2O: < 0.1 mg/mL (insoluble)

DMSO: 12 mg/mL (40.62 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.77 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3848 mL	16.9239 mL	33.8478 mL	169.2391 mL
5 mM	0.6770 mL	3.3848 mL	6.7696 mL	33.8478 mL
10 mM	0.3385 mL	1.6924 mL	3.3848 mL	16.9239 mL
20 mM	0.1692 mL	0.8462 mL	1.6924 mL	8.4620 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

Serotonin Receptor Pizotifen Inhibitor inhibit BC105 BC 105 5-hydroxytryptamine Receptor 5HTReceptor 5-HT Receptor 5HT Receptor 5-HT

Pizotifen

Pizotifen

Pizotifen 相关产品

产品介绍

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体内实验配液计算器

剂量转换

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