Umibecestat CNP520|cas:1387560-01-1|西域试剂

Umibecestat CNP520,99.88%

产品编号：Bellancom-119689| CAS NO：1387560-01-1| 分子式：C₁₉H₁₅ClF₇N₅O₂| 分子量：513.80

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-119689		￥4500.00	杭州北京（现货）
Bellancom-119689		￥8000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Umibecestat CNP520

产品介绍

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。

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. Umibecestat can be used for the research of alzheimer's disease.

体外研究

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.

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

体内研究

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.
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.

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

Animal Model:	Male rats (3-4 months old)
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
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.

体内研究

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

Animal Model:	Male rats (3-4 months old)
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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (194.63 mM; Need ultrasonic)

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
10 mM	0.1946 mL	0.9731 mL	1.9463 mL

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。

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)

参考文献