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Vortioxetine hydrobromide

Catalog No. T2395L CAS 960203-27-4

Synonyms: Vortioxetine (Lu AA21004) HBr, Vortioxetine 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).

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Vortioxetine hydrobromide Chemical Structure

Vortioxetine hydrobromide, CAS 960203-27-4

Pack Size	Availability	Price/USD
10 mg	In stock	$ 43.00
25 mg	In stock	$ 58.00
50 mg	In stock	$ 89.00
100 mg	In stock	$ 126.00
200 mg	In stock	$ 197.00
500 mg	In stock	$ 369.00
1 g	In stock	$ 531.00
1 mL * 10 mM (in DMSO)	In stock	$ 38.00

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Purity: 100%

Purity: 99.89%

Purity: 99.48%

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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	5-HT13A:3.7nM, 5-HT1A:15nM, SERT:1.6nM, 5-HT11B:33nM, 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.

Synonyms	Vortioxetine (Lu AA21004) HBr, Vortioxetine HBr, Lu AA21004 hydrobromide
Molecular Weight	379.36
Formula	C18H22N2S·HBr
CAS No.	960203-27-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 14 mg/mL (36.9 mM)

DMSO: 71 mg/mL (187.2 mM)

References and Literature

1. Bang-Andersen B, et al. J Med Chem, 2011, 54(9), 3206-3221. 2. Mørk A, et al. J Pharmacol Exp Ther, 2012, 340(3), 666-675. 3. Mørk A, et al. Pharmacol Biochem Behav, 2013, 105C, 41-50.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library GPCR Compound Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library EMA Approved Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Serotonin Receptor-Targeted Compound Library

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Keywords

Vortioxetine hydrobromide 960203-27-4 GPCR/G Protein Neuroscience 5-HT Receptor Serotonin Transporter Lu AA21004 Vortioxetine (Lu AA21004) HBr 5-HTT Vortioxetine HBr Lu AA 21004 Serotonin Receptor Inhibitor SLC6A4 Lu AA-21004 Hydrobromide Lu AA21004 hydrobromide Lu AA21004 Hydrobromide SERT Vortioxetine Vortioxetine Hydrobromide Lu AA 21004 Hydrobromide Lu AA-21004 inhibit 5-hydroxytryptamine Receptor inhibitor

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