Emixustat hydrochloride
Based on 1 Customer Validation
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).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.29%
- CAS. Nr.: 1141934-97-5
- Formel: C16H26ClNO2
- Molecular Weight:299.84
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Biologische Aktivität
IC50: 4.4 nM (Retinal Pigment Epithelium 65-kDa protein (RPE65))[4]
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1141934-97-5
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Appearance Solid
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Molecular Weight 299.84
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Formel C16H26ClNO2
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Color White to off-white
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SMILES
O[C@H](CCN)C1=CC(OCC2CCCCC2)=CC=C1.[H]Cl
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Synonyms
ACU-4429 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. 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]
[2]. Kubota R, 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. [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 (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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