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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $98 | 5 days | 5 days | |
| 5 mg | $226 | 5 days | 5 days | |
| 25 mg | $766 | 1-2 weeks | 1-2 weeks | |
| 50 mg | $996 | 1-2 weeks | 1-2 weeks | |
| 100 mg | $1,740 | 1-2 weeks | 1-2 weeks | |
| 1 mL x 10 mM (in DMSO) | $189 | 5 days | 5 days |
| 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. |
| Synonyms | ACU-4429 |
| Molecular Weight | 263.38 |
| Formula | C16H25NO2 |
| Cas No. | 1141777-14-1 |
| Smiles | NCC[C@@H](O)c1cccc(OCC2CCCCC2)c1 |
| Relative Density. | 1.065 g/cm3 (Predicted) |
| Storage | Powder: -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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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