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Diphenhydramine

Name: Diphenhydramine
Brand: TargetMol
SKU: T21419
Price: 150 CNY
Availability: InStock
Rating: 5 (10 reviews)

Synonyms: 苯海拉明, Syntedril, PM-255, PM255, PM 255, Debendrin, Dabylen

货号 T21419Cas号 58-73-1 一键复制产品信息纯度: 98.07%

很棒

Diphenhydramine (Syntedril) 是第一代具有抗胆碱能作用的H1 受体拮抗剂，它能透过血脑屏障。

Diphenhydramine

一键复制产品信息

很棒

纯度: 98.07%

货号 T21419Cas号 58-73-1

别名 苯海拉明, Syntedril, PM-255, PM255, PM 255, Debendrin, Dabylen

Diphenhydramine (Syntedril) 是第一代具有抗胆碱能作用的H1 受体拮抗剂，它能透过血脑屏障。

规格	价格	库存
200 mg	¥ 329	现货
500 mg	¥ 538	现货
1 mL x 10 mM (in DMSO)	¥ 150	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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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: 98.07%

颜色: 无色透明

性状: Liquid

资源下载: COA HNMR GC LCMS产品操作手册

产品介绍

Diphenhydramine AI Summary

Diphenhydramine exhibits a broad spectrum of pharmacological and bioactivity properties. It has a distribution volume of 4.5 L.kg-1 and demonstrates high plasma protein binding with a low unbound fraction (Fu = 0.22). The compound is highly ionized at a physiological pH of 7.4, with a pKa of 9.1. It shows notable lipophilicity with an eLog D value of 1.38. Pharmacokinetically, Diphenhydramine has a half-life of 31.05 hours in humans, with an apparent volume of distribution of 3.3 L.kg-1 and a high oral bioavailability of 79.0%. It exhibits a high unbound drug partitioning coefficient in the brain (Kp = 3.02), indicating substantial central nervous system penetration. Bioactivity-wise, Diphenhydramine shows potent antihistaminic activity, inhibiting histamine H1 receptor with an IC50 value of 1.0 nM in guinea pig ileum. It also exhibits significant anti-inflammatory and anti-allergic properties, reducing foot edema in rats and demonstrating protection in guinea pig anaphylaxis assays. The compound shows broad inhibitory activity against various enzymes and receptors, including histamine N-methyl-transferase (activity of 10.0 nM) and UGT1A4 enzyme. It also inhibits the binding of Batrachotoxinin [3H]BTX-B to voltage-dependent sodium channels with an IC50 of 6000.0 nM and exhibits 59.8% inhibition at 10 µM in the same assay. Diphenhydramine also demonstrates antiviral activity against SARS-CoV-2 with an IC50 value greater than 20000.0 nM for inhibiting virus-induced cytotoxicity in Vero-6 cells, and a 11.32% inhibition of SARS-CoV-2 3CL-Pro protease at 20µM. It shows potential as an anti-nociceptive agent, reducing scratching behaviors in mice models induced by histamine. Furthermore, Diphenhydramine inhibits various ion channels, including the human ERG potassium channel (IC50 = 26915.35 nM), and shows inhibitory effects on sodium and calcium currents in cardiac cells. It also demonstrates activity against a range of histamine, serotonin, and muscarinic receptors, indicating its diverse pharmacological profile. Despite its broad-spectrum activity, Diphenhydramine exhibits moderate liver toxicity and high metabolic stability in rat liver microsomes, with a half-life of 0.1133 hours and intrinsic clearance values indicative of rapid metabolism. These features make Diphenhydramine a compound of significant interest for potential therapeutic applications across various pathways and target sites..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Diphenhydramine (Syntedril), a first-generation antihistamine possessing antiemetic, antitussive, anticholinergic, and sedative properties, is mainly used in the treatment of allergies. Diphenhydramine is also used in the management of drug-induced parkinsonism and other extrapyramidal symptoms.
靶点活性	NMDAR:24.6 μM
别名	苯海拉明, Syntedril, PM-255, PM255, PM 255, Debendrin, Dabylen

化学信息

分子量	255.35
分子式	C₁₇H₂₁NO
CAS No.	58-73-1
Smiles	C(OCCN(C)C)(C1=CC=CC=C1)C2=CC=CC=C2
密度	1.024 g/cm3

储存&溶解度

存储

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

实际储存温度请以COA为准

溶解度信息

H2O: Insoluble

DMSO: 242.5 mg/mL (949.68 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.9162 mL	19.5810 mL	39.1619 mL	195.8097 mL
5 mM	0.7832 mL	3.9162 mL	7.8324 mL	39.1619 mL
10 mM	0.3916 mL	1.9581 mL	3.9162 mL	19.5810 mL
20 mM	0.1958 mL	0.9790 mL	1.9581 mL	9.7905 mL
50 mM	0.0783 mL	0.3916 mL	0.7832 mL	3.9162 mL
100 mM	0.0392 mL	0.1958 mL	0.3916 mL	1.9581 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

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

Inhibitor inhibit HistamineReceptor Histamine Receptor hay fever H1 receptor Endogenous Metabolite Diphenhydramine common cold allergy

Diphenhydramine

Diphenhydramine