Desvenlafaxine Succinate hydrate

製品コードS4112 バッチS411201

印刷

化学情報

Chemical Structure Synonyms WY 45233 Succinate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H25NO2.C4H6O4.H2O
分子量 399.48 CAS No. 386750-22-7
Solubility (25°C)* 体外 DMSO 80 mg/mL (200.26 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
0.5% methylcellulose 0.2% Tween 80
10.0mg/ml Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose+0.2% Tween 80 clear solution, and mix evenly to make it a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Desvenlafaxine Succinate hydrate (WY 45233) is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.
in vitro

Desvenlafaxine succinate is the succinate salt monohydrate of O-desmethylvenlafaxine, an active metabolite of venlafaxine. Desvenlafaxine Succinate is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, Desvenlafaxine Succinate inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine Succinate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine Succinate inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively.[1] Desvenlafaxine Succinate 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 Succinate, which could impact the metabolism of drugs metabolized via this enzyme. [2]
in vivo

Desvenlafaxine Succinate rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine Succinate significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. [1] Desvenlafaxine Succinate 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%.[2]
特徴 A major active metabolite of venlafaxine.

プロトコル(参考用のみ)

キナーゼアッセイ 5-HT Radioligand Membrane Binding Assay
Frozen membranes are suspended in binding buffer (50 mM Tris-HCl, 120 mM NaCl, and 5 mM KCl, pH 7.4) and prepared to approximately 5 μg of protein per 50 μl of aliquot. Binding reactions are run in 96-well OptiPlates. Cell membranes (50 μl) are added to each well of the reaction plate followed by 40 μl of binding buffer, 10 μl of test compound or buffer, or 50 μl of [3H]citalopram (1 nM final concentration). The [3H]citalopram is run at the approximate KD concentration, and 94 to 96% specific binding is achieved in this assay. Data from wells containing fluoxetine (10 μM) are used to define nonspecific hSERT membrane binding (minimum binding in the presence of a 5-HT reuptake inhibitor). All reaction wells receive 50 μl of wheat germ agglutinin scintillation proximity assay beads (containing 0.5 mg) made in 50 mM Tris-HCl, 120 mM NaCl, and 5 mM KCl, pH 7.4. The reaction plates are then incubated for a minimum of 1 h to reach equilibrium. The plates are then counted on a TopCount scintillation counter.
動物実験 動物モデル Male Sprague-Dawley rats
投薬量 30 mg/kg
投与方法 Oral

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Influence of Zuojin Pill on the Metabolism of Venlafaxine in Vitro and in Rats and Associated Herb-Drug Interaction [ Drug Metab Dispos, 2020, 48(10):1044-1052] PubMed: 32561594

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。