Venlafaxine
Based on 6 publication(s) in Google Scholar
Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.71%
- CAS 番号: 93413-69-5
- 分子式: C17H27NO2
- 分子量:277.40
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Venlafaxine
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>10000 nM
Compound: 1
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Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes
Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes
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[PMID: 20378347] |
| CHO | IC50 |
7340 nM
Compound: 3
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Inhibition of dopamine reuptake at human dopamine transporter expressed in CHO cells
Inhibition of dopamine reuptake at human dopamine transporter expressed in CHO cells
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[PMID: 20724153] |
| HEK293 | IC50 |
35 nM
Compound: 3
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Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells
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[PMID: 20724153] |
| HEK293 | IC50 |
>20 nM
Compound: 6
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Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
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[PMID: 24900709] |
| HEK293 | IC50 |
680 nM
Compound: 6
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Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis
Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis
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[PMID: 24900709] |
| HEK293 | IC50 |
15767 nM
Compound: Venlafaxine
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Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
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[PMID: 24974340] |
| HEK293 | IC50 |
36.1 nM
Compound: Venlafaxine
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Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
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[PMID: 24974340] |
| HEK293 | IC50 |
5722 nM
Compound: Venlafaxine
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Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
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[PMID: 24974340] |
| JAR | IC50 |
31 nM
Compound: 1, venlafaxine
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Inhibition of 5HT uptake at human SERT expressed in human JAR cells
Inhibition of 5HT uptake at human SERT expressed in human JAR cells
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[PMID: 18557608] |
| JAR | IC50 |
27 nM
Compound: 1
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Inhibition of human SERT expressed in human JAR cells
Inhibition of human SERT expressed in human JAR cells
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[PMID: 20378347] |
| MDCK | IC50 |
581 nM
Compound: 3
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Inhibition of norepinephrine reuptake at human NET expressed in MDCK cells
Inhibition of norepinephrine reuptake at human NET expressed in MDCK cells
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[PMID: 20724153] |
Venlafaxine (Wy 45030) dose-dependently inhibits binding of the serotonin transporter radioligand [3H]-paroxetine to membranes from cells transfected with the human 5-HT transporter with a Ki of 2.48 μM. Venlafaxine inhibits binding of the NE transporter ligand [3H]-nisoxetine to membranes from cells transfected with the human NE transporter with a Ki of 82 nM[1].
Venlafaxine inhibits ex vivo binding to rat 5-HT transporters and NE transporters with ED50 values of 2 and 54 mg/kg, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats weighing 180-230 grams[1]
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Dosage:10, 30, 100 mg/kg
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Administration:IP; one hour prior to p-chloramphetamine hydrochloride (p-CA; 10 mg/kg; i.p.)
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Result:Dose-dependently blocked the depletion of norepinephrine levels in rat hypothalamus induced by 6-OHDA (intracerebroventricularly; 50 μg/rat; one hour later), with ED50 values of 12 and 94 mg/kg, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 93413-69-5
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性状 Solid
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分子量 277.40
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分子式 C17H27NO2
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Color White to off-white
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SMILES
OC1(C(C2=CC=C(OC)C=C2)CN(C)C)CCCCC1
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別名
Wy 45030
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Water Res
Enhanced venlafaxine degradation in amorphous FeS2 under redox-dynamic aqueous environments: Critical role of citrate in electron utilization for boosted hydroxyl radical generation. [Abstract]2025 Oct 1;288(Pt B):124709. PMID: 41046790 -
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J Med Chem
Exploring Simple Drug Scaffolds from the Generated Database Chemical Space Reveals a Chiral Bicyclic Azepane with Potent Neuropharmacology. [Abstract]2025 Apr 24. PMID: 40274264 -
Neurosci Bull
Targeting 5-HT to Alleviate Dose-Limiting Neurotoxicity in Nab-Paclitaxel-Based Chemotherapy. [Abstract]2025 Jul;41(7):1229-1245. PMID: 40369268 -
J Agric Food Chem
Fluoride Stimulates Anxiety- and Depression-like Behaviors Associated with SIK2-CRTC1 Signaling Dysfunction. [Abstract]2021 Nov 17;69(45):13618-13627. PMID: 34735150 -
Int Immunopharmacol
Innovative role of the antidepressant imipramine in esophageal squamous cell carcinoma treatment: Promoting apoptosis and protective autophagy. [Abstract]2025 Jan 6:147:113969. PMID: 39764996
溶剤 & 溶解度
DMSO : 200 mg/mL (720.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bymaster FP, et al. Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology. 2001 Dec;25(6):871-80. [Content Brief]
[2]. Goeringer KE, et al. Postmortem tissue concentrations of venlafaxine. Forensic Sci Int. 2001 Sep 15;121(1-2):70-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6049 mL | 18.0245 mL | 36.0490 mL | 90.1226 mL |
| 5 mM | 0.7210 mL | 3.6049 mL | 7.2098 mL | 18.0245 mL | |
| 10 mM | 0.3605 mL | 1.8025 mL | 3.6049 mL | 9.0123 mL | |
| 15 mM | 0.2403 mL | 1.2016 mL | 2.4033 mL | 6.0082 mL | |
| 20 mM | 0.1802 mL | 0.9012 mL | 1.8025 mL | 4.5061 mL | |
| 25 mM | 0.1442 mL | 0.7210 mL | 1.4420 mL | 3.6049 mL | |
| 30 mM | 0.1202 mL | 0.6008 mL | 1.2016 mL | 3.0041 mL | |
| 40 mM | 0.0901 mL | 0.4506 mL | 0.9012 mL | 2.2531 mL | |
| 50 mM | 0.0721 mL | 0.3605 mL | 0.7210 mL | 1.8025 mL | |
| 60 mM | 0.0601 mL | 0.3004 mL | 0.6008 mL | 1.5020 mL | |
| 80 mM | 0.0451 mL | 0.2253 mL | 0.4506 mL | 1.1265 mL | |
| 100 mM | 0.0360 mL | 0.1802 mL | 0.3605 mL | 0.9012 mL |
Venlafaxine 関連分類
HY-B0196 関連分類
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