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Emixustat

Catalog No. T11188 CAS 1141777-14-1

Synonyms: ACU-4429

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

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Emixustat, CAS 1141777-14-1

Pack Size	Availability	Price/USD
2 mg	5 days	$ 98.00
5 mg	5 days	$ 226.00
25 mg	6-8 weeks	$ 766.00
50 mg	6-8 weeks	$ 996.00
100 mg	6-8 weeks	$ 1,740.00
1 mL * 10 mM (in DMSO)	5 days	$ 189.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Emixustat, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro. a novel visual cycle modulator.
Targets&IC50	Visual cycle isomerase:4.4 nM
In vitro	Emixustat strongly inhibits 11-cis-retinol production with an IC50 value of 232±3 nM.Emixustat potently inhibits isomerase activity in vitro (IC50=4.4 nM). Treatment of emixustat shows a concentration dependent reduction of 11-cis-ROL production .
In vivo	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).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.

Synonyms	ACU-4429
Molecular Weight	263.38
Formula	C16H25NO2
CAS No.	1141777-14-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 43 mg/mL (163.26 mM)

References and Literature

1. Bavik C, et al. Visual Cycle Modulation as an Approach toward Preservation of Retinal Integrity. PLoS One. 2015 May 13;10(5):e0124940. 2. Kiser PD, et al. Catalytic mechanism of a retinoid isomerase essential for vertebrate vision. Nat Chem Biol. 2015 Jun;11(6):409-15.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Emixustat 1141777-14-1 Others ACU-4429 ACU4429 ACU 4429 inhibitor inhibit

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