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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).

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Emixustat Chemical Structure

Emixustat Chemical Structure

CAS No. : 1141777-14-1

Size Price Stock Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 145 In-stock
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Oil
2 mg USD 100 In-stock
5 mg USD 150 In-stock
10 mg USD 240 In-stock
50 mg USD 595 In-stock
100 mg USD 950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

IC50: 4.4 nM (Retinal Pigment Epithelium 65-kDa protein (RPE65))[4]

In Vitro

Emixustat (0.1 nM - 10 μM, 1 h) concentration-dependently reduces the production of 11-cis-retinol, thereby inhibiting RPE65 activity[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

263.38

Formula

C16H25NO2

CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

O[C@H](CCN)C1=CC(OCC2CCCCC2)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7968 mL 18.9840 mL 37.9680 mL
5 mM 0.7594 mL 3.7968 mL 7.5936 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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