化学信息：
| 化学名 |
(R)-N-(3-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,2,4-thiadiazin-5-yl)-4-fluorophenyl)-5-fluoropicolinamide |
| 简称 |
MK-8931, BACE1/2 Inhibitor |
| 别名 |
Verubecestat, Beta-site APP cleaving enzyme 1/2 Inhibitor |
| 中文名 |
维罗司他 |
| 化学式 |
C17H17F2N5O3S |
| 分子量 |
409.41 |
| CAS号 |
1286770-55-5 |
| 纯度 |
>98% |
| 溶剂/溶解度 |
H2O insoluble; 11mg/ml in EtOH; ≥40.9 mg/ml in DMSO |
| 溶液配制 |
5mg加入1.221ml DMSO，或者每4.094mg加入1ml DMSO，配制成10mM溶液。 |
生物信息:
| 产品描述 |
Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor, which effectively reduces Aβ40 and has the potential inhibitory effect for Alzheimer's Disease. |
| 信号通路 |
Neural signaling pathway; Neurodegenerative disease; Alzheimer's disease |
| 靶点 |
Human BACE1 |
Mouse BACE1 |
BACE2 |
Aβ40 |
- |
| Ki |
2.2nM |
3.4nM |
0.38nM |
7.8nM |
- |
| 体外研究 |
Verubecestat is a potent inhibitor of both human and mouse BACE1, as well as purified human BACE2. It is also found to be an inhibitor of Ab40, Ab42, and sAPPb in human cells with similar potency. Moreover, verubecestat was essentially inactive with over 45,000-fold selectivity in the purified human aspartyl proteases cathepsin D, cathepsin E, and pepsin and had a very weak inhibitory effect on purified human renin with 15,000-fold selectivity. In addition, verubecestat was also found to have minimal or no activity against various tested receptors, ion channels, transporters, as well as enzymes [1-3]. |
| 体内研究 |
In both rats and monkeys, verubecestat could reduce plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42 and sAPPβ after acute and chronic administration. Moreover, the chronic treatment with verubecestat at exposures >40-fold higher than those tested in clinical trials did not cause many of the adverse effects previously reported in BACE inhibition. In rabbits and mice (but not in monkeys), fur hypopigmentation was found [1-3]. |
| 临床实验 |
Single and multiple doses of verubecestat were generally well tolerated and produced reductions in Aβ40, Aβ42, and sAPPβ in the CSF [1]. |
| 特征 |
- |
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 细胞实验 |
| 细胞系 |
- |
| 浓度 |
- |
| 处理时间 |
- |
| 方法 |
- |
| 动物实验 |
| 动物模型 |
Sprague-Dawley (SD) rats |
| 剂量 |
3 mg/kg (Pharmacokinetic Analysis) |
| 给药方式 |
IV or oral |
| 结果 |
Had a T1/2 of 1.9 hours, a CL of 46ml/min/kg, a Vss of 5.4L/kg, a Cmax of 0.27μM and a AUC of 1.1μM•h. |
包装清单：
| 产品编号 |
产品名称 |
包装 |
| SF1183-10mM |
Verubecestat (MK-8931) (BACE1/2抑制剂) |
10mM×0.2ml |
| SF1183-5mg |
Verubecestat (MK-8931) (BACE1/2抑制剂) |
5mg |
| SF1183-25mg |
Verubecestat (MK-8931) (BACE1/2抑制剂) |
25mg |
| SF1183-100mg |
Verubecestat (MK-8931) (BACE1/2抑制剂) |
100mg |
| － |
说明书 |
1份 |
保存条件：
-20℃保存，至少一年有效。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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