1141777-14-1
1141777-14-1 structure
- Name: Emixustat
- Chemical Name: (1R)-3-amino-1-[3-(cyclohexylmethoxy)phenyl]propan-1-ol
- CAS Number: 1141777-14-1
- Molecular Formula: C16H25NO2
- Molecular Weight: 263.37500
- Catalog: Research Areas Metabolic Disease
- Create Date: 2016-05-18 09:35:36
- Modify Date: 2024-01-02 12:57:51
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Emixustat, a novel visual cycle modulator, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro.
| Name | (1R)-3-amino-1-[3-(cyclohexylmethoxy)phenyl]propan-1-ol |
|---|---|
| Synonyms |
emixustat
unii-02dz1hbf0m acu 4229 |
| Description | Emixustat, a novel visual cycle modulator, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro. |
|---|---|
| Related Catalog | |
| Target |
IC50: 4.4 nM (visual cycle isomerase)[1] |
| In Vitro | Emixustat potently inhibits isomerase activity in vitro (IC50=4.4 nM). Treatment of emixustat shows a concentration dependent reduction of 11-cis-ROL production [1]. Emixustat strongly inhibits 11-cis-retinol production with an IC50 value of 232±3 nM[2]. |
| In Vivo | Emixustat reduces the production of visual chromophore (11-cis retinal) in wild-type mice following a single oral dose (ED50=0.18mg/kg). In albino mice, emixustat is shown to be effective in preventing photoreceptor cell death caused by intense light exposure. Pre-treatment with a single dose of emixustat (0.3 mg/kg) provids 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 reduces A2E levels by 60%( ED50=0.47 mg/kg). In the retinopathy of prematurity rodent model, treatment with emixustat during the period of ischemia and reperfusion injury produces a 30%reduction in retinal neovascularization (ED50=0.46mg/kg)[1]. |
| Animal Admin | Mice: Albino (BALB/c) mice are used to assess the effects of emixustat on protection from light damage. Mice are treated with a single dose of emixustat (0.3 mg/kg and 1.0 mg/kg). The effect of emixustat on the accumulation of A2E and lipofuscin autofluorescence is examined in Abca4-/- mice. Mice are treated with emixustat (3 months daily treatment, 0.3 or 3 mg/kg/day)[1]. |
| References |
| Molecular Formula | C16H25NO2 |
|---|---|
| Molecular Weight | 263.37500 |
| Exact Mass | 263.18900 |
| PSA | 55.48000 |
| LogP | 3.72820 |
| Storage condition | 2-8℃ |