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                同义名:
                    
                        
                            
                                Diphenhydramine (hydrochloride); DPH
                            
                        
                    
                
                
                
                    
                     
                
            
Diphenhydramine HCl 是一种组胺 H1 受体拮抗剂,常用于抗呕吐、止咳及过敏机制研究。
 
                                 
                                
                            

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| 产品名称 | H1 receptor ↓ ↑ | H2 receptor ↓ ↑ | H3 receptor ↓ ↑ | H4 receptor ↓ ↑ | Histamine receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Hydroxyzine 2HCl | 99+% | ||||||||||||||||||
| Cyclizine | ✔ | 97% | |||||||||||||||||
| Loratadine | + B(0)AT2, IC50: 4 μM | 98% | |||||||||||||||||
| Desloratadine | ++ Histamine H1 receptor, IC50: 51 nM | 98% | |||||||||||||||||
| Doxylamine succinate | ✔ | 99% | |||||||||||||||||
| Ebastine | ✔ | 98% | |||||||||||||||||
| Tripelennamine HCl | + H1 receptor, IC50: 30 μM | 98% | |||||||||||||||||
| Meclizine 2HCl | ✔ | 98% | |||||||||||||||||
| Chlorpheniramine maleate | +++ Histamine H1 receptor, IC50: 12 nM | 99% | |||||||||||||||||
| Diphenhydramine HCl | ✔ | 99% | |||||||||||||||||
| Alcaftadine | ++++ H1 receptor, pKi: 8.5 | ++ H2 receptor, pKi: 7.2 | 99%+ | ||||||||||||||||
| Fexofenadine HCl | ++ Histamine H1 receptor, IC50: 246 nM | 99%+ | |||||||||||||||||
| Bilastine | +++ H1 receptor, Ki: 44.15 nM | 98% | |||||||||||||||||
| Pemirolast potassium | ✔ | 98% | |||||||||||||||||
| Bepotastine besilate | + Histamine H1 receptor, pIC50: 5.7 | 98% | |||||||||||||||||
| Mizolastine | +++ Histamine H1 receptor, IC50: 47 nM | 98% | |||||||||||||||||
| Brompheniramine maleate | ✔ | 98% | |||||||||||||||||
| Carbinoxamine maleate salt | ✔ | 99+% | |||||||||||||||||
| Clemastine fumarate | ++++ Histamine H1 receptor, IC50: 3 nM | 98% | |||||||||||||||||
| Ketotifen fumarate salt | ✔ | 95% | |||||||||||||||||
| Rupatadine Fumarate | ++ Histamine H1 receptor, Ki: 102 nM | PAFR | 98% | ||||||||||||||||
| Famotidine | ✔ | 97% | |||||||||||||||||
| Roxatidine Acetate HCl | + Histamine H2 receptor, IC50: 3.2 μM | 98% | |||||||||||||||||
| Lafutidine | ✔ | 99% | |||||||||||||||||
| Cimetidine | ✔ | 98% | |||||||||||||||||
| Nizatidine | ++++ Histamine H2 receptor, IC50: 0.9 nM | AChE | 98% | ||||||||||||||||
| Ranitidine | ✔ | 96% | |||||||||||||||||
| Betahistine | + Histamine H3 receptor, IC50: 1.9 μM | 99% | |||||||||||||||||
| Ciproxifan maleate | +++ Histamine H3 receptor, IC50: 9.2 nM | 99%+ | |||||||||||||||||
| S 38093 | ++ human H3 receptor, Ki: 1.2 μM rat H3 receptor, Ki: 1.44 μM | 98% | |||||||||||||||||
| JNJ-7777120 | ++++ Histamine H4 receptor, Ki: 4.5 nM | 99% | |||||||||||||||||
| Azelastine HCl | ✔ | 98% | |||||||||||||||||
| Epinastine HCl | ✔ | 99% | |||||||||||||||||
| Levodropropizine | ✔ | 97% | |||||||||||||||||
| Cyproheptadine HCl | ✔ | 98% | |||||||||||||||||
| Hesperetin | ✔ | 97% | |||||||||||||||||
| Olopatadine HCl | ✔ | 98% | |||||||||||||||||
| Mianserin HCl | ✔ | 99+% | |||||||||||||||||
| Buclizine 2HCl | ✔ | 95% | |||||||||||||||||
| Latrepirdine 2HCl | ✔ | GluR | 99% | ||||||||||||||||
| Cetirizine 2HCl | ✔ | 98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 | 
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| 描述 | Diphenhydramine (DPH) Hydrochloride is most commonly used via oral, topical, intramuscular (IM) and intravenous (IV) routes for the palliation of pruritus, treatment of extrapyramidal symptoms, management of parkinsonism and for allergic reactions. Subcutaneous diphenhydramine injection is a safe alternative to oral and other parenteral routes, and may be particularly valuable in terminally ill patients, who are often unable to swallow and are without IV access[3]. IV administration of diphenhydramine prior to MCT (mast cell tumor) excision had no clear clinical cardiorespiratory benefits over placebo in isoflurane-anesthetized dogs[4]. Intravenous diphenhydramine hydrochloride given before initiation of midazolam and pethidine offers a significant Improvement of quality of moderate sedation during colonoscopy without increasing the number of sedation related complications[5]. | 
| Concentration | Treated Time | Description | References | |
| HEK293 cells expressing hTRPA1 | 1 mM | To test the effect of DPH on AITC-activated hTRPA1 currents. Results showed that 1 mM DPH completely suppressed outward currents while enhancing inward currents. | Cell Calcium. 2020 Sep;90:102245 | |
| HEK293 cells | 100 μM and 1 mM | To test the effect of DPH on TRPA1 channels expressed in HEK293 cells. Results showed that 100 μM DPH had no effect on basal currents, while 1 mM DPH partially suppressed basal currents. | Cell Calcium. 2020 Sep;90:102245 | |
| Chinese hamster ovary (CHO) cells | 1 mM | 30 minutes | To investigate the inhibitory effect of diphenhydramine on histamine-induced JNK phosphorylation, results showed that diphenhydramine completely inhibited histamine-induced JNK phosphorylation. | Int J Mol Sci. 2024 Mar 17;25(6):3395 | 
| Administration | Dosage | Frequency | Description | References | ||
| Female C57BL/6 mice | Experimental autoimmune encephalomyelitis (EAE) model | Intraperitoneal injection | 10 mg/kg | Daily for 15 days | To investigate the effect of Diphenhydramine hydrochloride on EAE development, results showed that the drug significantly delayed the onset of EAE and reduced behavioral scores, while also reducing inflammatory cell infiltration and white matter demyelination in the spinal cord. | J Neurosci. 2016 Aug 31;36(35):9253-66 | 
| Mice | Wild-type and knockout mice | Carotid artery perfusion | 1.4 μmol/L | 60 seconds | To evaluate the transport mechanism of Diphenhydramine at the blood-retinal barrier, finding that its transport is mainly mediated by a proton antiporter with a lower passive diffusion rate. | Br J Pharmacol. 2015 Oct;172(19):4714-25 | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 3.43mL 0.69mL 0.34mL | 17.13mL 3.43mL 1.71mL | 34.27mL 6.85mL 3.43mL | |
| CAS号 | 147-24-0 | 
| 分子式 | C17H22ClNO | 
| 分子量 | 291.81 | 
| SMILES Code | CN(CCOC(C1=CC=CC=C1)C2=CC=CC=C2)C.[H]Cl | 
| MDL No. | MFCD00012479 | 
| 别名 | Diphenhydramine (hydrochloride); DPH; Difenhydramine; Diphenhydramine hydrochloride | 
| 运输 | 蓝冰 | 
| InChI Key | PCHPORCSPXIHLZ-UHFFFAOYSA-N | 
| Pubchem ID | 8980 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place,Sealed in dry,2-8°C | 
| 溶解方案 | DMSO: 105 mg/mL(359.82 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 100 mg/mL(342.68 mM),配合低频超声助溶 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
 
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