货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S82084-5mg	≥98%	￥1490.00 S82084-5mg ￥1490.00 3-5天	0 货期：3-5天	-	-	-	-
S82084-10mg	≥98%	￥2390.00 S82084-10mg ￥2390.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S82084-5mg

≥98%

￥1490.00

货期：3-5天

S82084-10mg

≥98%

￥2390.00

货期：3-5天

产品描述：

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

靶点：

IC50: 4.4 nM (visual cycle isomerase);Others

体外研究：

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

体内研究：

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)

参考文献：

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.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.797 ml	18.984 ml	37.969 ml
5 mM	0.759 ml	3.797 ml	7.594 ml
10 mM	0.38 ml	1.898 ml	3.797 ml
50 mM	0.076 ml	0.38 ml	0.759 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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