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Lurasidone

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Catalog No. T21337Cas No. 367514-87-2
Alias SM-13496

Lurasidone (SM-13496) is an antagonist of dopamine D2 and 5-HT7 receptors (IC50 = 1.68 and 0.495 nM, respectively) and a partial agonist of the 5-HT1A receptor (IC50 = 6.75 nM).

Lurasidone

Lurasidone

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Purity: 99.91%
Catalog No. T21337Alias SM-13496Cas No. 367514-87-2
Lurasidone (SM-13496) is an antagonist of dopamine D2 and 5-HT7 receptors (IC50 = 1.68 and 0.495 nM, respectively) and a partial agonist of the 5-HT1A receptor (IC50 = 6.75 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$39In StockIn Stock
10 mg$53In StockIn Stock
25 mg$78In StockIn Stock
50 mg$98In StockIn Stock
100 mg$148In StockIn Stock
200 mg$217-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.91%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Lurasidone (SM-13496) is an antagonist of dopamine D2 and 5-HT7 receptors (IC50 = 1.68 and 0.495 nM, respectively) and a partial agonist of the 5-HT1A receptor (IC50 = 6.75 nM).
Targets&IC50
5-HT7 receptor:0.495 nM (IC50), 5-HT1A receptor:6.75 nM (IC50), D2 receptor:1.68 nM (IC50)
In vitro
Lurasidone is administered once daily within the range of 40-160 mg/day for schizophrenia and 20-120 mg/day for bipolar depression, and its pharmacokinetic profile requires administration with food.?In adult healthy subjects and patients, a 40 mg dose results in peak plasma concentrations in 1-3 h, a mean elimination half-life of 18 h (mostly eliminated in the feces), and apparent volume of distribution of 6173 L;?it is approximately 99 % bound to serum plasma proteins.?Lurasidone's pharmacokinetics are approximately dose proportional in healthy adults and clinical populations within the approved dosing range, and this was also found in a clinical study of children and adolescents.?Lurasidone is principally metabolized by cytochrome P450 (CYP) 3A4 with minor metabolites and should not be coadministered with strong CYP3A4 inducers or inhibitors.?Lurasidone does not significantly inhibit or induce CYP450 hepatic enzymes[2].
In vivo
In addition to its principal antagonist activity at dopamine D2 and serotonin 5-HT2A receptors, lurasidone has distinctive 5-HT7 antagonistic activity, and displays partial agonism at 5-HT1A receptors, as well as modest antagonism at noradrenergic α2A and α2C receptors.?Lurasidone is devoid of antihistaminic and anticholinergic activities[1].
SynonymsSM-13496
Chemical Properties
Molecular Weight492.68
FormulaC28H36N4O2S
Cas No.367514-87-2
SmilesO=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1C[C@@H]1CCCC[C@H]1CN1CCN(CC1)c1nsc2ccccc12
Relative Density.1.273 g/cm3
Storage & Solubility Information
Storagestore under nitrogen | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 17.83 mg/mL (36.19 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 1.5 mg/mL (3.04 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0297 mL10.1486 mL20.2972 mL101.4858 mL
5 mM0.4059 mL2.0297 mL4.0594 mL20.2972 mL
10 mM0.2030 mL1.0149 mL2.0297 mL10.1486 mL
20 mM0.1015 mL0.5074 mL1.0149 mL5.0743 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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