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Emixustat (Synonyms: ACU-4429)

Cat. No.: HY-19720
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.

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Emixustat Chemical Structure

Emixustat Chemical Structure

CAS No. : 1141777-14-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO $159 In-stock
2 mg $110 In-stock
5 mg $200 In-stock
10 mg $320 In-stock
50 mg $1100 In-stock
100 mg $1750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Emixustat:

  • Biological Activity

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  • Technical Information

  • References

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
NCT Number Sponsor Condition Start Date Phase
NCT01002950 Acucela Inc.|Otsuka Pharmaceutical Co., Ltd. Dry Age-related Macular Degeneration|Geographic Atrophy October 2009 Phase 2
NCT00942240 Acucela Inc.|Otsuka Pharmaceutical Co., Ltd. Healthy July 2009 Phase 1
NCT00703183 Acucela Inc. Healthy May 2008 Phase 1
NCT01802866 Acucela Inc.|Otsuka Pharmaceutical Co., Ltd. Geographic Atrophy February 2013 Phase 2|Phase 3
NCT01002950 Acucela Inc.|Otsuka Pharmaceutical Co., Ltd. Dry Age-related Macular Degeneration|Geographic Atrophy October 2009 Phase 2
NCT00942240 Acucela Inc.|Otsuka Pharmaceutical Co., Ltd. Healthy July 2009 Phase 1
NCT00703183 Acucela Inc. Healthy May 2008 Phase 1
NCT01802866 Acucela Inc.|Otsuka Pharmaceutical Co., Ltd. Geographic Atrophy February 2013 Phase 2|Phase 3
NCT03033108 Acucela Inc. Stargardt Disease January 2017 Phase 2
NCT02753400 Acucela Inc. Proliferative Diabetic Retinopathy April 2016 Phase 2
NCT02130531 Acucela Inc. Geographic Atrophy|Age-Related Macular Degeneration April 2014 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Animal Administration
[1]

Emixustat is prepared in water.

Mouse: 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
Molecular Weight

263.38

Formula

C₁₆H₂₅NO₂

CAS No.

1141777-14-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 43 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Emixustat
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