Emixustat (ACU-4429) (Synonyms: ACU-4429) |
| Catalog No.GC31373 |
Emixustat (ACU-4429) es un modulador del ciclo visual de moléculas pequeñas que inhibe el complejo isomerasa.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1141777-14-1
Sample solution is provided at 25 µL, 10mM.
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Emixustat (ACU-4429) es un modulador del ciclo visual de moléculas pequeñas que inhibe el complejo isomerasa. Como inhibidor de la isomerasa del ciclo visual, el valor de IC50 es de 4.4 nM[1].
Emixustat inhibe fuertemente la producción de 11-cis-retinol con un valor de IC50 de 232±3 nM[2]. Una reducción dependiente de la concentración de la producción de 11-cis-ROL (i.e., inhibición de la actividad de la isomerasa RPE65) por emixustat(10-5 to 10-10 M)[1].
Se descubrió que emixustat(0.01-3.0 mg/kg; p.o) reduce la producción de cromóforo visual (retiniano 11-cis) en ratones de tipo salvaje después de una sola dosis oral (ED50 = 0.18 mg/kg) [1]. En 40 subjetos (edad media, 38 años) Emixustat (n = 30) (5, 10, 20, 30, o 40 mg; 14 días) se absorbió rápidamente (mediana T(máx), 3.0-5 horas) y se eliminó fácilmente (t media(1/2), 4.6-7.9 horas), y la C media(máx) generalmente aumentó en proporción a la dosis. Los eventos adversos sistémicos fueron mínimos[3]. Emixustat reduce significativamente la permeabilidad después de la reperfusión de isquemia (IR) en la permeabilidad vascular en ratones[4].
References:
[1]. Bavik C, Henry SH, 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. PMID: 25970164; PMCID: PMC4430241.
[2]. Kiser PD, Zhang J, 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. Epub 2015 Apr 20. PMID: 25894083; PMCID: PMC4433804.
[3].Kubota R, Al-Fayoumi S, et,al. Phase 1, dose-ranging study of emixustat hydrochloride (ACU-4429), a novel visual cycle modulator, in healthy volunteers. Retina. 2014 Mar;34(3):603-9. doi: 10.1097/01.iae.0000434565.80060.f8. PMID: 24056528.
[4].Dreffs A, Lin CM, et,al. All-trans-Retinaldehyde Contributes to Retinal Vascular Permeability in Ischemia Reperfusion. Invest Ophthalmol Vis Sci. 2020 Jun 3;61(6):8. doi: 10.1167/iovs.61.6.8. PMID: 32492112; PMCID: PMC7415894.
| Experimentos con animales [1]: | |
Modelos animales | Ratones BALB/c (8 semanas) |
Método de preparación | Los ratones BALB/c adaptados a la oscuridad (12 horas) (8 semanas, n = 4/grupo) fueron dosificados por vía oral con emixustat (0.01-3.0 mg/kg) o vehículo (agua). A las 4 horas posteriores a la dosis, los animales fueron fotoblanqueados (luz blanca de 5000 lux, 10 min) sin anestesia ni midriáticos, devueltos a la oscuridad durante 2 horas y luego sacrificados bajo luz roja. |
Forma de dosificación | 0.01-3.0 mg/kg; p.o |
Áreas de aplicación | Se descubrió que mixustat reduce la producción de cromóforo visual (retina 11-cis) en ratones de tipo salvaje después de una sola dosis oral (ED50 = 0.18 mg/kg). |
References: [1]. Bavik C, Henry SH,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. PMID: 25970164; PMCID: PMC4430241. | |
| Cas No. | 1141777-14-1 | SDF | |
| Sinónimos | ACU-4429 | ||
| Canonical SMILES | O[C@H](CCN)C1=CC(OCC2CCCCC2)=CC=C1 | ||
| Formula | C16H25NO2 | M.Wt | 263.38 |
| Solubility | DMSO : ≥ 43 mg/mL (163.26 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7968 mL | 18.984 mL | 37.968 mL |
| 5 mM | 759.4 μL | 3.7968 mL | 7.5936 mL |
| 10 mM | 379.7 μL | 1.8984 mL | 3.7968 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50%
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