去甲文拉法辛, 去甲肾上腺素转运体抑制剂

Adrenergic Receptor Inhibitors
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货号 (SKU) 包装规格 是否现货 价格 数量
D409248-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 WY 45233 Succinate | Phenol, 4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Desvenlafaxine
生化机理 地文拉法辛(WY 45233 Succinate)是一种血清素(5-HT)和去甲肾上腺素(NE)再摄取抑制剂,其Ki值分别为 40.2 nM 和 558.4 nM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 去甲肾上腺素转运体抑制剂
产品介绍

邻去甲基文拉法辛是文拉法辛的主要活性代谢产物。


Information

Desvenlafaxine Desvenlafaxine (WY 45233 Succinate) is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with K i of 40.2 nM and 558.4 nM, respectively.
In vitro

Desvenlafaxine is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, desvenlafaxine inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. Desvenlafaxine has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Induction of CYP3A4 is also possible with desvenlafaxine, which could impact the metabolism of drugs metabolized via this enzyme.

In vivo

Desvenlafaxine rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. Desvenlafaxine exhibits a linear and dose-proportional pharmacokinetic single-dose profile in a dose range from 100 to 600 mg/day. The absolute bioavailability of the oral formulation is 80.5%.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

ALogP 2.796
HBD Count 1
Rotatable Bond 4

关联靶点(人)

SLC6A2 Tclin 钠依赖性去甲肾上腺素转运体(Sodium-dependent noradrenaline transporter) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
SLC6A3 Tclin 钠依赖性多巴胺转运体(Sodium-dependent dopamine transporter) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
SLC6A4 Tclin 钠依赖性血清素转运体(Sodium-dependent serotonin transporter) (4 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CN(C)CC(C1=CC=C(O)C=C1)C2(O)CCCCC2
分子量 263.38
Reaxy-Rn 4234613
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4234613&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility 37
DMSO(mM) Max Solubility 140.48
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 4234613
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4234613&ln=

技术规格说明书

Concentration(Compounding value) 9-11(mmol/L)
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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