| Identification | Back Directory | [Name]
(R)-3-amino-1-(3-(cyclohexylmethoxy)phenyl)propan-1-ol | [CAS]
1141777-14-1 | [Synonyms]
Incemixustat
(R)-3-amino-1-(3-(cyclohexylmethoxy)phenyl)propan-1-ol
Benzenemethanol, α-(2-aminoethyl)-3-(cyclohexylmethoxy)-, (αR)- | [Molecular Formula]
C16H25NO2 | [MDL Number]
MFCD26961089 | [MOL File]
1141777-14-1.mol | [Molecular Weight]
263.38 |
| Chemical Properties | Back Directory | [Boiling point ]
430.9±40.0 °C(Predicted) | [density ]
1.065±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 43 mg/mL (163.26 mM) | [form ]
Oil | [pka]
14.01±0.20(Predicted) | [color ]
Colorless to light yellow |
| Hazard Information | Back Directory | [Uses]
Emixustat is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat is also a visual cycle modulator, capable of regulating visual cycle activity by inhibiting retinol isomerization, and holds potential for studying vision disorders such as age-related macular degeneration (AMD)[1][2][3][4]. | [in vivo]
Emixustat (1-10 mg/kg, oral administration, single dose, or twice daily for 6 days; 1 mg/kg, i.p., measurement after 30-60 minutes) reduced cation influx and oxygen consumption in the retinas of brown Norway rats under dark adaptation conditions[3].
Emixustat (0.03-3.0 mg/kg, intravenous injection, once daily for 5 days) inhibits neovascularization and protects the retina in the oxygen-induced retinopathy mouse model[4]. | Animal Model: | Brown norway rats (200-300 g, 3 months old)[3] | | Dosage: | 1, 5 or 10 mg/kg | | Administration: | Oral gavage (p.o.), single dose (1, 10 mg/kg), 2 hours followed by 4 hours of dark adaptation, or twice a day for 6 days (5 mg/kg) | | Result: | Reduced the conductance of the retinal cation channels after dark adaptation. |
| Animal Model: | Brown norway rats (200-300 g, 3 months old)[3] | | Dosage: | 1 mg/kg | | Administration: | Intravenous injection (i.v.), retinal PO2 was measured 30-60 min later | | Result: | Reduced the oxygen consumption during dark adaptation. |
| Animal Model: | Oxygen-induced retinopathy (OIR) mice model (BALB/c and 129/Sv / C57BL/6 mixed background) | | Dosage: | 0.03, 0.1, 0.3, 1.0, 3.0 mg/kg | | Administration: | Intravenous injection (i.v.), once daily for 5 days | | Result: | Dose-dependently reduced retinal neovascularization. |
| [References]
[1] Bavik C, et al. Visual Cycle Modulation as an Approach toward Preservation of Retinal Integrity. PLoS One. 2015 May 13;10(5):e0124940. DOI:10.1371/journal.pone.0124940
[2] Kiser PD, et al. Catalytic mechanism of a retinoid isomerase essential for vertebrate vision. Nat Chem Biol. 2015 Jun;11(6):409-15. DOI:10.1038/nchembio.1799
[3] Kubota R, et al. Emixustat Reduces Metabolic Demand of Dark Activity in the Retina. Invest Ophthalmol Vis Sci. 2019 Nov 1;60(14):4924-4930. DOI:10.1167/iovs.19-28194
[4] Bavik C, et al. Visual Cycle Modulation as an Approach toward Preservation of Retinal Integrity. PLoS One. 2015 May 13;10(5):e0124940. DOI:10.1371/journal.pone.0124940 |
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