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Emixustat hydrochloride  (Synonyms: ACU-4429 hydrochloride)

Cat. No.: HY-19720A Purity: 99.59%
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Emixustat (ACU-4429) hydrochloride is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat hydrochloride 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 hydrochloride Chemical Structure

Emixustat hydrochloride Chemical Structure

CAS No. : 1141934-97-5

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Based on 1 publication(s) in Google Scholar

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Emixustat hydrochloride Related Antibodies

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Description

Emixustat (ACU-4429) hydrochloride is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat hydrochloride 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.

Emixustat hydrochloride Related Antibodies
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

299.84

Formula

C16H26ClNO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 44 mg/mL (146.74 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3351 mL 16.6756 mL 33.3511 mL
5 mM 0.6670 mL 3.3351 mL 6.6702 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

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

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 (sealed storage, away from moisture). 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 1 mM 3.3351 mL 16.6756 mL 33.3511 mL 83.3778 mL
5 mM 0.6670 mL 3.3351 mL 6.6702 mL 16.6756 mL
10 mM 0.3335 mL 1.6676 mL 3.3351 mL 8.3378 mL
15 mM 0.2223 mL 1.1117 mL 2.2234 mL 5.5585 mL
20 mM 0.1668 mL 0.8338 mL 1.6676 mL 4.1689 mL
25 mM 0.1334 mL 0.6670 mL 1.3340 mL 3.3351 mL
30 mM 0.1112 mL 0.5559 mL 1.1117 mL 2.7793 mL
40 mM 0.0834 mL 0.4169 mL 0.8338 mL 2.0844 mL
50 mM 0.0667 mL 0.3335 mL 0.6670 mL 1.6676 mL
60 mM 0.0556 mL 0.2779 mL 0.5559 mL 1.3896 mL
80 mM 0.0417 mL 0.2084 mL 0.4169 mL 1.0422 mL
100 mM 0.0334 mL 0.1668 mL 0.3335 mL 0.8338 mL
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Emixustat hydrochloride Related Classifications

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.

Keywords:

Emixustat1141934-97-5ACU-4429ACU4429ACU 4429OthersOxygen-induced retinopathy (OIR) mice modelBrown norway ratsage-related macular degenerationInhibitorinhibitorinhibit

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