1. Others
  2. Others
  3. Emixustat

Emixustat (Synonyms: ACU-4429)

Cat. No.: HY-19720 Purity: 99.05%
Handling Instructions

Emixustat, a novel visual cycle modulator, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro.

For research use only. We do not sell to patients.

Emixustat Chemical Structure

Emixustat Chemical Structure

CAS No. : 1141777-14-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 191 In-stock
Estimated Time of Arrival: December 31
2 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
10 mg USD 384 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Emixustat:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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.

IC50 & 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].

Clinical Trial
Molecular Weight

263.38

Formula

C₁₆H₂₅NO₂

CAS No.

1141777-14-1

SMILES

O[[email protected]](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)

*"≥" 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
10 mM 0.3797 mL 1.8984 mL 3.7968 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% EtOH    90% corn oil

    Solubility: ≥ 3 mg/mL (11.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

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].

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

EmixustatACU-4429ACU4429ACU 4429OthersInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Emixustat
Cat. No.:
HY-19720
Quantity:
MCE Japan Authorized Agent: