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Vortioxetine hydrobromide
🥰Excellent
Catalog No. T2395LCas No. 960203-27-4
Alias Vortioxetine HBr, Vortioxetine (Lu AA21004) HBr, Lu AA21004 hydrobromide
Vortioxetine hydrobromide (Lu AA21004 hydrobromide) is a serotonin (5-HT) modulator and stimulator (SMS), inhibits 5-HT1A/1B/3A/7 receptor and SERT (IC50: 15/33/3.7/19/1.6 nM).
Vortioxetine hydrobromide
🥰Excellent
Purity: 100%
Catalog No. T2395LAlias Vortioxetine HBr, Vortioxetine (Lu AA21004) HBr, Lu AA21004 hydrobromideCas No. 960203-27-4
Vortioxetine hydrobromide (Lu AA21004 hydrobromide) is a serotonin (5-HT) modulator and stimulator (SMS), inhibits 5-HT1A/1B/3A/7 receptor and SERT (IC50: 15/33/3.7/19/1.6 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $35 | In Stock | |
| 50 mg | $53 | In Stock | |
| 100 mg | $76 | In Stock | |
| 500 mg | $221 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $29 | In Stock |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Vortioxetine hydrobromide (Lu AA21004 hydrobromide) is a serotonin (5-HT) modulator and stimulator (SMS), inhibits 5-HT1A/1B/3A/7 receptor and SERT (IC50: 15/33/3.7/19/1.6 nM). |
| Targets&IC50 | SERT:1.6nM, 5-HT11B:33nM, 5-HT13A:3.7nM, 5-HT1A:15nM, 5-HT7:19nM |
| In vitro | Subcutaneous injection of Lu AA21004 (2.5-10.0 mg/kg) into the medial prefrontal cortex and ventral hippocampal area of rats was found to elevate extracellular levels of 5-HT, DA, and NA. A specific dose of Lu AA21004 (5 mg/kg) targeting the rats’ ventral hippocampal region resulted in a 200% increase in extracellular 5-HT levels. Additionally, administration of Lu AA21004 (at doses of 5 and 10 mg/kg) showed a significant elevation in ACh levels to 224% and 204% respectively, 20 minutes post-injection. This compound, when administered to the ventral hippocampal area of awake rats at doses of 5 and 10 mg/kg, enhanced extracellular 5-HT levels, and a 3-day treatment of the medial prefrontal cortex with Lu-AA21004 (at 5 and 10 mg/kg) substantially raised the basal levels of 5-HT. Furthermore, Lu AA21004 (10 mg/kg) notably decreased pain perception in rats. In terms of pharmacokinetics within rats, Lu-AA21004 exhibited a liver clearance rate of 7.1 (L/h)/kg and an oral bioavailability of 16%. Lastly, Lu AA21004 dose-dependently affected the rats' Bezold-Jarisch reflex by inhibiting transient bradycardia (ED50: 0.11 mg/kg). |
| In vivo | Lu AA21004 acts as an agonist for the h5-HT1B receptor, with an EC50 value of 460 nM and demonstrating 22% intrinsic activity in whole-cell assays. It inhibits recombinant human cytochrome P450 enzymes CYP1A2, CYP2C9, CYP2D6, and CYP3A4 with IC50 values of 40 μM, 39 μM, 9.8 μM, and 10 μM, respectively. Furthermore, Lu AA21004 binds to the r5-HT7 receptor with a Ki value of 200 nM in vitro whole-cell cAMP assays and functions as a competitive antagonist with an IC50 of 2 μM. |
| Kinase Assay | Assay of MEK Kinase Activity: Anti-MEK1 antibody is used to immunoprecipitate MEK1 molecules. MEK kinase activity is measured as the ability of immuno-isolated MEK1 to activate recombinant ERK1 in a coupled assay using MBP as the end point of the assay. Phosphorylated MBP is resolved on a 14% SDS-PAGE gel and vacuum-dried before exposure to X-ray film. |
| Alias | Vortioxetine HBr, Vortioxetine (Lu AA21004) HBr, Lu AA21004 hydrobromide |
| Molecular Weight | 379.36 |
| Formula | C18H22N2S·HBr |
| Cas No. | 960203-27-4 |
| Smiles | c1c(c(cc(c1)C)C)Sc1ccccc1N1CCNCC1.Br |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 14 mg/mL (36.9 mM) DMSO: 45 mg/mL (118.62 mM)  | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Keywords
Vortioxetine hydrobromideVortioxetine HydrobromideVortioxetineSLC6A4SERTSerotoninTransporterSerotonin TransporterSerotonin ReceptorLu AA-21004 HydrobromideLu AA21004 HydrobromideLu AA-21004Lu AA21004Lu AA 21004 HydrobromideLu AA 21004Inhibitorinhibit5-hydroxytryptamine Receptor5-HTT5HTReceptor5-HT Receptor5HT Receptor
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