| Verubecestat (MK-8931)BACE1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.56%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
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Chemical structure
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| Cas No. | 1286770-55-5 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (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 | ||
| Canonical SMILES | O=C(NC1=CC=C(C([C@@](C)(N=C(N2C)N)CS2(=O)=O)=C1)F)C3=CC=C(C=N3)F | ||
| Formula | C17H17F2N5O3S | M.Wt | 409.41 |
| Solubility | ≥40.9mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Ki: 2.2 and 3.4 nM for human and mouse Bace1, respectively
Verubecestat (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].
Clinical trial: Single and multiple doses of verubecestat were generally well tolerated and produced reductions in Aβ40, Aβ42, and sAPPβ in the CSF [1].
Reference:[1] Kennedy ME et al. The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer"s disease patients. Sci Transl Med.2016 Nov 2;8(363):363ra150.
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buffer P1：除去RNA
buffer P2：裂解细胞
buffer P3：沉淀DNA
buffer WA、buffer WB：都是洗涤液（这两个之间有什么区别我也不清楚）
TE：溶解DNA.
这个与琼脂糖电泳有关。提取的DNA分子量很大，可能在40K到100K左右。也有可能在这个范围。但普通的琼脂糖电泳。在大分子的时候根本分别不出来。如果你有DL15000的MARKER你就知道，象那个一万与一万五和条带差别很近。
1、DNA提取问题：现在核算提取试剂盒大部分都是吸附柱法,相信你应该不会操作错误,如果提取之后进行核酸定量结果很低的话,试着再最后一步溶解核算的时候把水稍微加温（37℃就可以了）,溶解时间稍微长一些,然后再离心的时候采用分次离心,比如开始你用200ul溶解的话,你可以分两次用100ul水溶解离心,这样可以提高DNA的产率.
2、电泳问题：如果你核酸定量浓度不低的话就考虑电泳问题,电泳的时候加上1kb的marker,如果marker跑不出来说明你凝胶有问题,一般只要marker跑出来了,DNA浓度又比较高,而没有条带这样的现象很少见,DNA提取比较简单而且相当稳定,本人当时做甲基化提取的DNA有一次拿出来电泳忘了放回冰箱了,结果大夏天的在外面放了一天,心怀忐忑的进行了一次电泳,结果条带依然给力,一点都没有降解.
不懂得请别粘贴那些有的没的，浪费资源
采用的给全部分
