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Emixustat

CAS No. 1141777-14-1

Emixustat( ACU-4429 )

Catalog No. M10502 CAS No. 1141777-14-1

Emixustat (ACU-4429) is a first in class small-molecule inhibitor of the visual cycle isomerase (RPE65) with IC50 of 4.4 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Emixustat
  • Note
    Research use only, not for human use.
  • Brief Description
    Emixustat (ACU-4429) is a first in class small-molecule inhibitor of the visual cycle isomerase (RPE65) with IC50 of 4.4 nM.
  • Description
    Emixustat (ACU-4429) is a first in class small-molecule inhibitor of the visual cycle isomerase (RPE65) with IC50 of 4.4 nM; reduces the production of visual chromophore (11-cis retinal) in wild-type mice following a single oral dose (ED50 = 0.18 mg/kg).Other Indication Phase 3 Clinical
  • 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 . Emixustat strongly inhibits 11-cis-retinol production with an IC50 value of 232±3 nM.
  • 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 auto fluorescence 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).
  • Synonyms
    ACU-4429
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Other Targets
  • Research Area
    Other Indications
  • Indication
    Other Disease

Chemical Information

  • CAS Number
    1141777-14-1
  • Formula Weight
    263.3752
  • Molecular Formula
    C16H25NO2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 43 mg/mL
  • SMILES
    C1CCC(CC1)COC2=CC=CC(=C2)C(CCN)O
  • Chemical Name
    Benzenemethanol, α-(2-aminoethyl)-3-(cyclohexylmethoxy)-, (αR)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Kiser PD, et al. Nat Chem Biol. 2015 Jun;11(6):409-15. 2. Bavik C, et al. PLoS One. 2015 May 13;10(5):e0124940. 3. Zhang J, et al. J Clin Invest. 2015 Jul 1;125(7):2781-94.
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