Ambeed.cn

首页 / 抑制剂/激动剂 / / / Desvenlafaxine

去甲文拉法辛 /Desvenlafaxine {[allProObj[0].p_purity_real_show]}

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.

Desvenlafaxine 化学结构 CAS号:93413-62-8
Desvenlafaxine 化学结构
CAS号:93413-62-8
Desvenlafaxine 3D分子结构
CAS号:93413-62-8
Desvenlafaxine 化学结构 CAS号:93413-62-8
Desvenlafaxine 3D分子结构 CAS号:93413-62-8
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]}
{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} 现货 咨询 - +
购物车0 收藏 询单

Desvenlafaxine 纯度/质量文件 产品仅供科研

货号:A105155 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

全球学术期刊中引用的产品

Cell, 2024, 101755. Ambeed. [ A399663 ]
EMBO J., 2024. Ambeed. [ A295334 ]
JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]
JMC, 2024. Ambeed. [ A210558 , A1518164 ]
Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]
更多 >
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 (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

98%
Venlafaxine 98%
Fluvoxamine maleate 99%
Iloperidone 98%
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 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 98%
Fluoxetine HCl 99.5%
Paroxetine hydrochloride AChR 97%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

98%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

99%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
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%
Palonosetron 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

98%
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron hydrochloride dihydrate 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

98%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

+++

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-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 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

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。

Desvenlafaxine 生物活性

靶点
  • 5-HT

    5-HT, Ki:40.2 nM

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].

Desvenlafaxine 临床研究

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 <<

Desvenlafaxine 参考文献

[1]Sopko MA Jr, Ehret MJ, Grgas M. Desvenlafaxine: another "me too" drug? Ann Pharmacother. 2008 Oct;42(10):1439-46.

[2]Deecher DC, Beyer CE, et al.Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65.

[3]Deecher DC, Beyer CE, Johnston G, et al. Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006;318(2):657‐665

[4]Sopko MA Jr, Ehret MJ, Grgas M. Desvenlafaxine: another "me too" drug?. Ann Pharmacother. 2008;42(10):1439‐1446

Desvenlafaxine 实验方案

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

Desvenlafaxine 技术信息

CAS号93413-62-8
分子式C16H25NO2
分子量 263.375
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
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

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

动物实验配方

0.5% methylcellulose+0.2% Tween 80+water 30 mg/mL suspension

Ambeed 相关网站 Ambeed.cn Ambeed.com
Ambeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
  • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    Ambeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务,不为任何个人或者非科研性质用途提供服务。