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- 文献和实验
- 技术资料
- 库存:
45
- 英文名:
Verubecestat (MK-8931)
- CAS号:
1286770-55-5
- 供应商:
上海莼试
- 保存条件:
Store at -20°C
- 规格:
5mg 25mg 100mg 500mg 1g
分子式:C19H18F5N5O5S
分子量:523.43
溶解度:≥ 40.9mg/mL in DMSO
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
Ki: 2.2 and 3.4 nM for human and mouse Bace1, respectivelyVerubecestat (MK-8931) is a BACE1 inhibitor.β-Amyloid (Aβ) peptides are regarded to be involved in the etiology of AD. BACE1 is required for the Aβ production, and BACE1 inhibition is therefore an promising target for the AD treatment.In vitro: Verubecestat has been identified as a potent inhibitor of both human and mouse Bace1 and verubecestat could also inhibit the production of Ab40, Ab42, and sAPPb in human cells with similar potency. Verubecestat was also found to be a potent inhibitor of purified human BACE2. 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 inhibitor of 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].In vivo: Verubecestat could reduce plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAPPβ after acute and chronic administration to both rats and monkeys. Moreover, the chronic treatment of rats and monkeys with verubecestat at exposures >40-fold higher than those tested in clinical trials did not cause many of the adverse effects previously reported to BACE inhibition. In rabbits and mice but not in monkeys, fur hypopigmentation was found [1].
商品属性:
| 货号 | CS-01Y77321 | 规格 | 5mg 25mg 100mg 500mg 1g |
| CAS号 | 1286770-55-5 | 分子量 | 523.43 |
| 含量 | >99.50% | 别名 | N/A |
| 分子式 | C19H18F5N5O5S | 化学名 | (R)-5-fluoro-N-(4-fluoro-3-(3-imino-2,5-dimethyl-1,1-dioxido-1,2,4-thiadiazinan-5-yl)phenyl)picolinamide 2,2,2-trifluoroacetate |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
抗逆滴加序列
每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
反应时间及温度
加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
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1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。
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[3H](+)MK801 Radioligand Binding Assay at the N‐Methyl‐D‐Aspartate Receptor
receptor. This protocol takes advantage of one of the most potent and specific ligands that bind to this receptor, in this case [3 H](+)MK801. Importantly, this assay can detect and differentiate agonists and antagonists that bind to the glycine site
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