1. Neuronal Signaling
  2. Beta-secretase
  3. Umibecestat

Umibecestat  (Synonyms: CNP520)

目录号: HY-119689 纯度: 99.88%
COA 产品使用指南

Umibecestat (CNP520) 是一种 β 位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂, 在人 BACE-1 和鼠 BACE-1 中的 IC50 值分别为 11 nM 和 10 nM。Umibecestat 可用于阿尔茨海默病的研究。

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Umibecestat Chemical Structure

Umibecestat Chemical Structure

CAS No. : 1387560-01-1

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5 mg ¥3500
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10 mg ¥5250
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Customer Review

查看 Beta-secretase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively[1]. Umibecestat can be used for the research of alzheimer's disease.

IC50 & Target

IC50: 11 nM (human BACE-1), 10 nM (mouse BACE-1)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
3 nM
Compound: 5; CNP-520
Inhibition of BACE1 in CHO cells expressing human APP assessed as reduction in amyloidbeta (1 to 40 residues) level incubated for 24 hrs by immunoassay method
Inhibition of BACE1 in CHO cells expressing human APP assessed as reduction in amyloidbeta (1 to 40 residues) level incubated for 24 hrs by immunoassay method
[PMID: 30709653]
体外研究
(In Vitro)

Umibecestat (CNP520) is a potent BACE-1 inhibitor that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D[1].

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

体内研究
(In Vivo)

Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows a dose-dependent effects on Aβ40 and a long duration of action in both rat brain and CSF[1].
Umibecestat (CNP520) (3.1 mg/kg; oral administration; 7 days) shows a > 75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days[1].

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

Animal Model: Male rats (3-4 months old)[1]
Dosage: 1.5 mg/kg (3 μM/kg)-51.3 mg/kg (100 μM/kg)
Administration: Given by oral gavage; 72 hours
Result: Reduced 89.3±4.5% Aβ40 at the highest dose in brain tissue, and 50% lowering of rat brain Aβ40 (ED50) was 2.4±0.31 mg/kg. Reduced ~50% Aβ40 at a single oral 30 μM/kg (15.4 mg/kg) dose after 24 hours in both rat brain and CSF。
Animal Model: 3-month-old beagle dogs[1]
Dosage: 3.1 mg/kg (6 μM/kg)
Administration: Oral administration; 7 days
Result: Both Aβ40 and Aβ42 concentrations in CSF showed a > 75% reduction at 12-48 h after dosing and returned slowly to baseline over the next 7 days.
Clinical Trial
分子量

513.80

Formula

C19H15ClF7N5O2

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, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (194.63 mM; 超声助溶; 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 1.9463 mL 9.7314 mL 19.4628 mL
5 mM 0.3893 mL 1.9463 mL 3.8926 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 (protect from light)。-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

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 (protect from light)。-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 1.9463 mL 9.7314 mL 19.4628 mL 48.6571 mL
5 mM 0.3893 mL 1.9463 mL 3.8926 mL 9.7314 mL
10 mM 0.1946 mL 0.9731 mL 1.9463 mL 4.8657 mL
15 mM 0.1298 mL 0.6488 mL 1.2975 mL 3.2438 mL
20 mM 0.0973 mL 0.4866 mL 0.9731 mL 2.4329 mL
25 mM 0.0779 mL 0.3893 mL 0.7785 mL 1.9463 mL
30 mM 0.0649 mL 0.3244 mL 0.6488 mL 1.6219 mL
40 mM 0.0487 mL 0.2433 mL 0.4866 mL 1.2164 mL
50 mM 0.0389 mL 0.1946 mL 0.3893 mL 0.9731 mL
60 mM 0.0324 mL 0.1622 mL 0.3244 mL 0.8110 mL
80 mM 0.0243 mL 0.1216 mL 0.2433 mL 0.6082 mL
100 mM 0.0195 mL 0.0973 mL 0.1946 mL 0.4866 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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Umibecestat
目录号:
HY-119689
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