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Emixustat

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Catalog No. T11188Cas No. 1141777-14-1
Alias ACU-4429

Emixustat, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro. a novel visual cycle modulator.

Emixustat

Emixustat

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Catalog No. T11188Alias ACU-4429Cas No. 1141777-14-1
Emixustat, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro. a novel visual cycle modulator.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$985 days5 days
5 mg$2265 days5 days
25 mg$7661-2 weeks1-2 weeks
50 mg$9961-2 weeks1-2 weeks
100 mg$1,7401-2 weeks1-2 weeks
1 mL x 10 mM (in DMSO)$1895 days5 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
Emixustat, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro. a novel visual cycle modulator.
Targets&IC50
Visual cycle isomerase:4.4 nM
In vitro
Emixustat strongly inhibits 11-cis-retinol production with an IC50 value of 232±3 nM.Emixustat potently inhibits isomerase activity in vitro (IC50=4.4 nM). Treatment of emixustat shows a concentration dependent reduction of 11-cis-ROL production .
In vivo
Pre-treatment with a single dose of emixustat (0.3 mg/kg) provides a 50% protective effect against light-induced photoreceptor cell loss, while higher doses (1-3 mg/kg) are nearly 100% effective. In Abca4-/- mice, chronic (3-month) emixustat treatment markedly reduces lipofuscin autofluorescence and lowers A2E levels by 60% (ED50=0.47 mg/kg). In the retinopathy of prematurity rodent model, emixustat administered during ischemia and reperfusion injury results in a 30% reduction in retinal neovascularization (ED50=0.46 mg/kg). Emixustat reduces the production of visual chromophore (11-cis retinal) in wild-type mice after a single oral dose (ED50=0.18 mg/kg). In albino mice, emixustat effectively prevents photoreceptor cell death caused by intense light exposure.
SynonymsACU-4429
Chemical Properties
Molecular Weight263.38
FormulaC16H25NO2
Cas No.1141777-14-1
SmilesNCC[C@@H](O)c1cccc(OCC2CCCCC2)c1
Relative Density.1.065 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 43 mg/mL (163.26 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.7968 mL18.9840 mL37.9680 mL189.8398 mL
5 mM0.7594 mL3.7968 mL7.5936 mL37.9680 mL
10 mM0.3797 mL1.8984 mL3.7968 mL18.9840 mL
20 mM0.1898 mL0.9492 mL1.8984 mL9.4920 mL
50 mM0.0759 mL0.3797 mL0.7594 mL3.7968 mL
100 mM0.0380 mL0.1898 mL0.3797 mL1.8984 mL

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In Vivo Formulation Calculator (Clear solution)

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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Dose Conversion

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Tech Support

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