货号:A105155
                
                同义名:
                    
                        
                            o-去甲文拉法辛
                            
                             / O-Desmethylvenlafaxine; DVS 233
                            
                        
                    
                
                
                
                    
                     
                
            
Desvenlafaxine inhibits serotonin(5-HT) and norepinephrine (NE) reuptake with Ki of 40.2 nM and 558.4 nM, respectively.
 
                                 
                                
                            

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| 产品名称 | 5-HT ↓ ↑ | 5-HT1 ↓ ↑ | 5-HT2 ↓ ↑ | 5-HT3 ↓ ↑ | 5-HT5 ↓ ↑ | 5-HT6 ↓ ↑ | 5-HT7 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Desvenlafaxine | ++ 5-HT, Ki: 40.2 nM | 98% | |||||||||||||||||
| Lamotrigine | + 5-HT (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM | 98% | |||||||||||||||||
| Venlafaxine | ✔ | 99% | |||||||||||||||||
| Fluvoxamine maleate | ✔ | 99% | |||||||||||||||||
| Iloperidone | ✔ | 99% | |||||||||||||||||
| Ziprasidone HCl | ✔ | 98+% | |||||||||||||||||
| Atomoxetine HCI | + 5-HT, Ki: 77 nM | 98% | |||||||||||||||||
| Dapoxetine HCl | ✔ | 97% | |||||||||||||||||
| Trazodone | ✔ | 98+% | |||||||||||||||||
| Clomipramine HCl | ✔ | 98% | |||||||||||||||||
| Mirtazapine | ✔ | 99+% | |||||||||||||||||
| Escitalopram oxalate | +++ 5-HT, Ki: 0.89 nM | 97% | |||||||||||||||||
| Duloxetine | ✔ | 97% | |||||||||||||||||
| Sertraline HCl | ++ 5-HT, Ki: 13 nM | 98% | |||||||||||||||||
| Citalopram HBr | +++ serotonin reuptake, IC50: 1.8 nM | 98% | |||||||||||||||||
| Latrepirdine 2HCl | ✔ | GluR | 99% | ||||||||||||||||
| Fluoxetine HCl | ✔ | 99.5% | |||||||||||||||||
| Paroxetine HCl | ✔ | AChR | 99% | ||||||||||||||||
| BMY 7378 | ++ 5-HT1D, pIC50: 5.9 5-HT1A, pIC50: 6.4 | + 5-HT2, pIC50: 5.5 | 97% | ||||||||||||||||
| Flibanserin | +++ 5-HT1A, Ki: 1 nM | + 5-HT2A, Ki: 49 nM | 95% | ||||||||||||||||
| LY310762 | + 5-HT1D, Ki: 249 nM | 99%+ | |||||||||||||||||
| Cyclobenzaprine HCI | ✔ | 99% | |||||||||||||||||
| Blonanserin | +++ 5-HT2, Ki: 3.98 nM | 99% | |||||||||||||||||
| Cyproheptadine HCl | ++++ 5-HT2, IC50: 0.6 nM | 99+% | |||||||||||||||||
| Olanzapine | ✔ | 99+% | |||||||||||||||||
| Pimavanserin hemitartrate | +++ 5-HT2A, pIC50: 8.7 | 99% | |||||||||||||||||
| Ketanserin | +++ 5-HT2C (Rat), Ki: 50 nM 5-HT2C (Human), Ki: 2.5 nM | 99%+ | |||||||||||||||||
| Loxapine succinate | ++ 5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM | 98% | |||||||||||||||||
| Agomelatine | ✔ | 98% | |||||||||||||||||
| Clozapine | ✔ | 98% | |||||||||||||||||
| Amitriptyline | + 5-HT2, Ki: 235 nM | SERT | 99% | ||||||||||||||||
| PRX-08066 maleate | +++ 5-HT2B, IC50: 3.4 nM | 98+% | |||||||||||||||||
| RS-127445 | ++++ 5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5 | 99%+ | |||||||||||||||||
| Sarpogrelate HCl | ++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM | 98% | |||||||||||||||||
| Tropisetron | ✔ | 99% | |||||||||||||||||
| Ramosetron HCl | ++++ 5-HT3 receptor, Ki: 0.091 nM | 98% | |||||||||||||||||
| Ondansetron | ✔ | 99% | |||||||||||||||||
| Granisetron | ✔ | 98% | |||||||||||||||||
| Alosetron HCl | ✔ | 98% | |||||||||||||||||
| Ondansetron HCl dihydrate | ✔ | 98% | |||||||||||||||||
| VUF10166 | ++++ 5-HT3AB, Ki: 22 nM 5-HT3A, Ki: 0.04 nM | 99%+ | |||||||||||||||||
| Azasetron HCl | ++++ 5-HT3, IC50: 0.33 nM | 99% | |||||||||||||||||
| Asenapine maleate | +++ 5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6 | ++++ 5-HT2C, pKi: 10.46 5-HT2A, pKi: 9.75 | +++ 5-HT5A, pKi: 8.84 | ++++ 5-HT6, pKi: 9.6 | ++++ 5-HT7, pKi: 9.94 | 97% | |||||||||||||
| Risperidone | ++ 5-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 nM | ++++ 5-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 nM | + 5-HT5A, Ki: 206 nM | ++ 5-HT7, Ki: 6.6 nM | 98% | ||||||||||||||
| SB 271046 HCl | +++ 5-HT6, pKi: 8.92 | 99%+ | |||||||||||||||||
| Intepirdine | ++++ 5-HT6, pKi: 9.63 | 99%+ | |||||||||||||||||
| SB-269970 HCl | ++ 5-HT7, pKi: 8.3 | 98+% | |||||||||||||||||
| BRL 15572 | ++ 5-HT1D, pKi: 6 5-HT1B, pKi: 6.1 | ++ 5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2 | + 5-HT6, pKi: 5.9 | + 5-HT7, pKi: 6.3 | 95% | ||||||||||||||
| 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 | 
 | 
| 描述 | Biogenic amines such as serotonin (5-HT), norepinephrine (NE), and dopamine (DA) are neurotransmitters found in areas of the central nervous system (CNS) known to be important for regulation of cognitive function, mood, thermo-regulation, pain sensation, sexual function, and various aspects of endocrine function related to homeostasis. Desvenlafaxine exhibits inhibitory activity of serotonin (5-HT) and norepinephrine (NE) reuptake with Ki of 40.2 and 558.4 nM, respectively. Desvenlafaxine inhibited the uptake of [3H]5-HT at the hSERT with a mean IC50 value of 47.3 ± 19.4 nM. In addition, the IC50 value of desvenlafaxine for [3H]NE uptake was 531.3 ± 113.0 nM. Acute oral administration of desvenlafaxine (30 mg/kg) did not significantly alter concentrations of 5-HT in the hypothalamus. However, pretreatment with WAY-100635 (5-HT1A antagonist, 0.3 mg/kg s.c.), which did not alter 5-HT levels on its own, resulted in a significant 78% increase in extracellular 5-HT levels in the rat hypothalamus. In contrast, acute administration of desvenlafaxine, when given alone, produced a significant increase in NE concentrations[3]. The response and remission rates of depression at 8 weeks for the 50-mg dose of desvenlafaxine are 51-63% and 31-45%, respectively[4]. | 
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 | 
| NCT00797966 | Major Depressive Disorder | Phase 2 | Completed | - | - | 
| NCT00797966 | - | Completed | - | - | |
| NCT01916824 | Major Depressive Disorder ... 展开 >> Healthy Controls 收起 << | Phase 4 | Completed | - | United States, Georgia ... 展开 >> Emory Mood and Anxiety Disorders Program Atlanta, Georgia, United States, 30322 收起 << | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 3.80mL 0.76mL 0.38mL | 18.98mL 3.80mL 1.90mL | 37.97mL 7.59mL 3.80mL | |
| CAS号 | 93413-62-8 | 
| 分子式 | C16H25NO2 | 
| 分子量 | 263.38 | 
| SMILES Code | C1=CC(=CC=C1O)C(CN(C)C)C2(CCCCC2)O | 
| MDL No. | MFCD00871934 | 
| 别名 | o-去甲文拉法辛 ;O-Desmethylvenlafaxine; DVS 233; MDD-XR; (±)-O-Desmethyl Venlafaxine; WY 45233 Succinate | 
| 运输 | 蓝冰 | 
| InChI Key | KYYIDSXMWOZKMP-UHFFFAOYSA-N | 
| Pubchem ID | 125017 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, room temperature | 
| 溶解方案 | DMSO: 50 mg/mL(189.84 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 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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