Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

Lusaperidone

Catalog No. T11894Cas No. 214548-46-6
Alias R107474

Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.

Lusaperidone

Lusaperidone

Purity: 99.64%
Catalog No. T11894Alias R107474Cas No. 214548-46-6
Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.
Pack SizePriceAvailabilityQuantity
1 mg$133In Stock
5 mg$328In Stock
10 mg$529In Stock
25 mg$1,090In Stock
50 mg$1,850In Stock
100 mg$2,720In Stock
Bulk & Custom
Add to Cart
Questions
View More

Related Compound Libraries of "Lusaperidone"

Select Batch
Purity:99.64%
Contact us for more batch information
Resource Download
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
Description
Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.
Targets&IC50
α2B-adrenoceptor (human):1 nM (Ki), α2A-adrenoceptor:2.8 nM (Kb,human), α2C-adrenoceptor:4.4 nM (Kb,human), α2A-adrenoceptor:0.13 nM (Ki), H5-HT7 receptor:5 nM(Ki), α2C-adrenoceptor:0.15 nM(Ki)
In vitro
Lusaperidone exhibits subnanomolar affinity for α2A and α2C adrenergic receptors (Ki=0.13 and 0.15 nM, respectively) and demonstrates nanomolar affinity for hα2B adrenergic receptors and h5-HT7 receptors (Ki=1 and 5 nM, respectively). It interacts weakly (Ki values ranging between 81 and 920 nM) with dopamine-hD2L, -hD3, and -hD4, h5-HT1D-, h5-HT1F-, h5-HT2A-, h5-HT2C-, and h5-HT5A receptors. Lusaperidone, tested up to 10 μM, interacts only at micromolar concentrations or not at all with any of the other receptor or transporter binding sites tested in this study. Furthermore, Lusaperidone has been demonstrated to reverse the clonidine-induced inhibition of cyclic AMP production mediated by human α2A and α2C adrenoceptors expressed in cell lines (Kb is 2.8 and 4.4 nM, respectively) and acts as a full antagonist on both receptor subtypes[1].
In vivo
Lusaperidone occupies the α2A and α2C adrenergic receptors with an ED50 of 0.014 mg/kg sc (0.009-0.019) and 0.026 mg/kg sc (0.022-0.030), respectively. The uptake of R107474 is very rapid after in vivo intravenous administration, reaching maximum concentration in most tissues, including the brain, within 5 minutes of tracer injection[1].
AliasR107474
Chemical Properties
Molecular Weight359.42
FormulaC22H21N3O2
Cas No.214548-46-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 1 mg/mL (2.78 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7823 mL13.9113 mL27.8226 mL139.1130 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
%Tween 80
%ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Related Tags: buy Lusaperidone | purchase Lusaperidone | Lusaperidone cost | order Lusaperidone | Lusaperidone chemical structure | Lusaperidone in vivo | Lusaperidone in vitro | Lusaperidone formula | Lusaperidone molecular weight