Vortioxetine (Lu AA21004) HBr

Catalog No.S8021

Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

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In DMSO USD 410 In stock
USD 147 In stock
USD 997 In stock
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Vortioxetine (Lu AA21004) HBr Chemical Structure

Vortioxetine (Lu AA21004) HBr Chemical Structure
Molecular Weight: 379.36

Validation & Quality Control

Quality Control & MSDS

Product Information

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  • Research Area
  • Inhibition Profile

Product Description

Biological Activity

Description Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
Targets SERT [1] 5-HT3A [1] 5-HT1A [1] 5-HT7 [1] 5-HT1B [1]
IC50 1.6 nM(Ki) 3.7 nM(Ki) 15 nM(Ki) 19 nM(Ki) 33 nM(Ki)
In vitro Lu-AA21004 inhibits recombinant human CYP1A2, CYP2C9, CYP2D6 and CYP3A4 with IC50 of 40 μM, 39 μM, 9.8 μM and 10 μM, respectively. [1] Lu AA21004 is a partial h5-HT1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Lu AA21004 binds to the r5-HT7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay. [2]
In vivo For Lu-AA21004 the hepatic clearances and oral bioavailabilities in rats are found to be 7.1 (L/h)/kg and 16%. Lu-AA21004 (2.5 mg/kg, 5 mg/kg, or 10 mg/kg sc) increases the extracellular levels of 5-HT in the ventral hippocampus in conscious rats. Lu-AA21004 (5 mg/kg, or 10 mg/kg sc) also results in significantly higher basal levels of 5-HT in the medial prefrontal cortex (mPFC) after 3 days of treatment. Lu-AA21004 occupies SERT by 43% and 57% after 3 days of treatment with 5 mg/kg or 10 mg/kg in the rat medial prefrontal cortex. [1] Lu AA21004 dose-dependent occupies 5-HT1B receptor and the SERT with ED50 of 3.2 mg/kg and 0.4 mg/kg in rats one hour after subcutaneous administration. Lu AA21004 affects the Bezold-Jarisch reflex in the rat dose dependently, inhibiting transient bradycardia with ED50 of 0.11 mg/kg. Lu AA21004 (2.5-10.0 mg/kg s.c.) increases extracellular levels of 5-HT, DA, and NA in the medial prefrontal cortex and in the ventral hippocampus in rats. Lu AA21004 (5 mg/kg s.c.) increases in the extracellular levels of 5-HT (200%) in the ventral hippocampus of rats with 41% occupancy at the SERT. Lu AA21004 (7.8 mg/kg s.c.) significantly decreases the immobility time in the FSL rats but not in the FRL rats. Lu AA21004 (8.0 mg/kg p.o.) produces an increase in social interaction as well as a small, but significant, increase in locomotor activity in rats. Lu AA21004 (7.9 mg/kg s.c.) shows a dose-dependent anxiolytic-like effect in the conditioned fear assay in rats. [2] Vortioxetine (10 mg/kg) significantly increases freezing 60 min before acquisition in male Sprague-Dawley rats, suggesting enhanced contextual memory formation during acquisition and/or consolidation. Vortioxetine (5 mg/kg) also causes increased freezing rates during retention, an effect that reached statistical significance by post hoc tests. Vortioxetine (2.5 mg/kg or 5 mg/kg) prior to acquisition shows average exploration times of 29s and 33s for the novel object, respectively. Vortioxetine (10 mg/kg) significantly reduces nociception in rats, assessed as increased paw withdrawal latency. Vortioxetine at 5 and 10 mg/kg increases the levels of ACh to 224% and 204% of baseline 20 min after injection. [3]
Features A multimodal antidepressant.

Protocol(Only for Reference)

Kinase Assay: [1]

h5-HT3A Binding Affinity Assay [3H]Granisetron (1 nM) binding to h5-HT3A receptors is evaluated in membranes from a HEK-293 cell line stably expressing the hHT3A receptor. Nonspecific binding is measured in the presence of 10 μM bemesetron. After incubation, the membrane preparations are rapidly filtered under a vacuum using glass-fiber filters. Lu-AA21004 are tested at least three times over a 6 log concentration range. IC50 values are determined by nonlinear regression analysis using Hill equation curve fitting, and Ki values are calculated based on the Cheng−Prusoff equation.

Animal Study: [1]

Animal Models Rats
Formulation 10% hydroxypropyl-β-cyclodextrin
Dosages 10 mg/kg
Administration Subcutaneous

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Bang-Andersen B, et al. J Med Chem, 2011, 54(9), 3206-3221.

[2] M?rk A, et al. J Pharmacol Exp Ther, 2012, 340(3), 666-675.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-06-27)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02234362 Not yet recruiting Depression|Menopause|Vasomotor Disturbance|Hot Flashes|Sleep Massachusetts General Hospital|Takeda Pharmaceuticals Nor  ...more Massachusetts General Hospital|Takeda Pharmaceuticals North America, Inc. June 2015 Phase 4
NCT02454426 Not yet recruiting Major Depressive Disorder|Coronary Artery Disease Thomas Jefferson University|Takeda June 2015 Phase 0
NCT02395510 Recruiting Panic Disorder Siyan Clinical Corporation May 2015 Phase 4
NCT02389816 Recruiting Major Depressive Disorder Takeda April 2015 Phase 3
NCT02386488 Completed Pharmacokinetics H. Lundbeck A/S March 2015 Phase 1

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Chemical Information

Download Vortioxetine (Lu AA21004) HBr SDF
Molecular Weight (MW) 379.36
Formula

C18H22N2S.HBr

CAS No. 960203-27-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 76 mg/mL (200.33 mM)
Ethanol 17 mg/mL (44.81 mM)
Water <1 mg/mL (<1 mM)
In vivo 15% Captisol, pH 9 10 mg/mL
* <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.
Chemical Name Piperazine, 1-[2-[(2,4-dimethylphenyl)thio]phenyl]-, hydrobromide (1:1)

Tech Support & FAQs

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