Emixustat
Based on 1 Customer Validation
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).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.17%
- No. CAS: 1141777-14-1
- Fòrmula: C16H25NO2
- Peso molecular:263.38
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
IC50: 4.4 nM (Retinal Pigment Epithelium 65-kDa protein (RPE65))[4]
In Vitro
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Brown norway rats (200-300 g, 3 months old)[3]
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Dosage:1, 5 or 10 mg/kg
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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)
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Result:Reduced the conductance of the retinal cation channels after dark adaptation.
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Animal Model:Brown norway rats (200-300 g, 3 months old)[3]
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Dosage:1 mg/kg
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Administration:Intravenous injection (i.v.), retinal PO2 was measured 30-60 min later
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Result:Reduced the oxygen consumption during dark adaptation.
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Animal Model:Oxygen-induced retinopathy (OIR) mice model (BALB/c and 129/Sv / C57BL/6 mixed background)
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Dosage:0.03, 0.1, 0.3, 1.0, 3.0 mg/kg
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Administration:Intravenous injection (i.v.), once daily for 5 days
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Result:Dose-dependently reduced retinal neovascularization.
Chemical Information
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No. CAS 1141777-14-1
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Appearance Oil
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Peso molecular 263.38
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Fòrmula C16H25NO2
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Color Colorless to light yellow
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SMILES
O[C@H](CCN)C1=CC(OCC2CCCCC2)=CC=C1
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Synonyms
ACU-4429
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
Ethanol : 100 mg/mL (379.68 mM; Need ultrasonic)
DMSO : ≥ 43 mg/mL (163.26 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (11.39 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (11.39 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 3 mg/mL (11.39 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bavik C, et al. Visual Cycle Modulation as an Approach toward Preservation of Retinal Integrity. PLoS One. 2015 May 13;10(5):e0124940. [Content Brief]
[2]. Kiser PD, et al. Catalytic mechanism of a retinoid isomerase essential for vertebrate vision. Nat Chem Biol. 2015 Jun;11(6):409-15. [Content Brief]
[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. [Content Brief]
[4]. Bavik C, et al. Visual Cycle Modulation as an Approach toward Preservation of Retinal Integrity. PLoS One. 2015 May 13;10(5):e0124940. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 3.7968 mL | 18.9840 mL | 37.9680 mL | 94.9199 mL |
| 5 mM | 0.7594 mL | 3.7968 mL | 7.5936 mL | 18.9840 mL | |
| 10 mM | 0.3797 mL | 1.8984 mL | 3.7968 mL | 9.4920 mL | |
| 15 mM | 0.2531 mL | 1.2656 mL | 2.5312 mL | 6.3280 mL | |
| 20 mM | 0.1898 mL | 0.9492 mL | 1.8984 mL | 4.7460 mL | |
| 25 mM | 0.1519 mL | 0.7594 mL | 1.5187 mL | 3.7968 mL | |
| 30 mM | 0.1266 mL | 0.6328 mL | 1.2656 mL | 3.1640 mL | |
| 40 mM | 0.0949 mL | 0.4746 mL | 0.9492 mL | 2.3730 mL | |
| 50 mM | 0.0759 mL | 0.3797 mL | 0.7594 mL | 1.8984 mL | |
| 60 mM | 0.0633 mL | 0.3164 mL | 0.6328 mL | 1.5820 mL | |
| 80 mM | 0.0475 mL | 0.2373 mL | 0.4746 mL | 1.1865 mL | |
| 100 mM | 0.0380 mL | 0.1898 mL | 0.3797 mL | 0.9492 mL |
Emixustat Related Classifications
HY-19720 Related Classifications
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