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Emixustat hydrochloride  (Synonyms: ACU-4429 hydrochloride)

目录号: HY-19720A 纯度: 99.29%
COA 产品使用指南

Emixustat (ACU-4429) hydrochloride 是具口服活性的 RPE65 抑制剂,IC50 值为 4.4 nM。Emixustat hydrochloride 也是视觉周期调节剂,可通过抑制视黄醇异构化来调节视觉周期活动,有望用于研究视力疾病,如年龄相关性黄斑变性 (AMD)。

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Emixustat hydrochloride Chemical Structure

Emixustat hydrochloride Chemical Structure

CAS No. : 1141934-97-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1814
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2 mg ¥1100
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5 mg ¥1500
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10 mg ¥2400
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50 mg ¥5950
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Customer Review

Other Forms of Emixustat hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)[1][2][3][4].

IC50 & Target

IC50: 4.4 nM (Retinal Pigment Epithelium 65-kDa protein (RPE65))[4]

体外研究
(In Vitro)

Emixustat (0.1 nM - 10 μM, 1 小时) 以浓度依赖的方式减少 11-顺式视黄醇的产生,即抑制 RPE65 活性[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Emixustat (1-10 mg/kg,口服,单次给药,或每天给药两次,持续 6 天;1 mg/kg,静脉注射,30-60 分钟后测量) 在暗适应条件下减少了褐色挪威大鼠视网膜的阳离子流入和氧气消耗[3]
Emixustat (0.03-3.0 mg/kg,静脉注射,一天一次持续 5 天) 在氧诱导的视网膜病变小鼠模型中抑制新生血管生成,对视网膜起保护作用[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Brown norway rats (200-300 g, 3 months old)[3]
Dosage: 1, 5 or 10 mg/kg
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)
Result: Reduced the conductance of the retinal cation channels after dark adaptation.
Animal Model: Brown norway rats (200-300 g, 3 months old)[3]
Dosage: 1 mg/kg
Administration: Intravenous injection (i.v.), retinal PO2 was measured 30-60 min later
Result: Reduced the oxygen consumption during dark adaptation.
Animal Model: Oxygen-induced retinopathy (OIR) mice model (BALB/c and 129/Sv / C57BL/6 mixed background)
Dosage: 0.03, 0.1, 0.3, 1.0, 3.0 mg/kg
Administration: Intravenous injection (i.v.), once daily for 5 days
Result: Dose-dependently reduced retinal neovascularization.
Clinical Trial
分子量

299.84

Formula

C16H26ClNO2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 44 mg/mL (146.74 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3351 mL 16.6756 mL 33.3511 mL
5 mM 0.6670 mL 3.3351 mL 6.6702 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Emixustat hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Emixustat hydrochloride
目录号:
HY-19720A
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