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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $98 | 5 days | |
5 mg | $226 | 5 days | |
25 mg | $766 | 1-2 weeks | |
50 mg | $996 | 1-2 weeks | |
100 mg | $1,740 | 1-2 weeks | |
1 mL x 10 mM (in DMSO) | $189 | 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. |
Alias | ACU-4429 |
Molecular Weight | 263.38 |
Formula | C16H25NO2 |
Cas No. | 1141777-14-1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 43 mg/mL (163.26 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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