Saquinavir mesylate
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Saquinavir是有效的HIV蛋白酶抑制剂,对HIV-1和HIV-2蛋白酶的Ki值分别为0.12和小于0.1 nM[1]。
HIV蛋白酶是成熟病毒释放和病毒复制所必需的逆转录病毒天冬氨酸蛋白酶[2]。 HIV蛋白酶在适当的位点切割合成的多肽生成HIV病毒的成熟蛋白质。 HIV-1蛋白酶是一个有吸引力的治疗艾滋病(AIDS)的靶标。
Saquinavir是一个过渡态抑制剂,可结合到HIV蛋白酶的活性位点,从而防止多肽的切割[1]。Saquinavir抑制p55(HIV-1的gag多聚蛋白)裂解为p24,p24是慢性感染CEM细胞的病毒结构蛋白[2]。小鼠中,同时施加50 mg/kg的ritonavir将20 mg/kg saquinavir的生物利用度增加了325倍。Ritonavir可防止CYP3A将saquinavir代谢为无活性的形式。
Saquinavir也抑制原代培养的人皮层神经元中内源性Aβ40的水平。50或100 μM的saquinavir显著降低TCA可溶的细胞外组分的生成。Saquinavir减少人神经元中Aβ的产生,50 μM的抑制率达到90%。与对照组相比,300 μM的saquinavir表现出高达6、30、32和48%的BACE1活性抑制[3]。
参考文献:
1.Roberts NA, Martin JA, Kinchington D, Broadhurst AV, Craig JC, Duncan IB, Galpin SA, Handa BK, Kay J, Krohn A et al: Rational design of peptide-based HIV proteinase inhibitors. Science 1990, 248(4953):358-361.
2.Davies DR: The structure and function of the aspartic proteinases. Annu Rev Biophys Biophys Chem 1990, 19:189-215.
3.Lan X, Kiyota T, Hanamsagar R, Huang Y, Andrews S, Peng H, Zheng JC, Swindells S, Carlson GA, Ikezu T: The effect of HIV protease inhibitors on amyloid-beta peptide degradation and synthesis in human cells and Alzheimer's disease animal model. J Neuroimmune Pharmacol 2012, 7(2):412-423
.Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 766.95 |
Cas No. | 149845-06-7 |
Formula | C39H54N6O8S |
Synonyms | Invirase; Ro 31-8959/003 |
Solubility | insoluble in H2O; ≥6.71 mg/mL in EtOH with gentle warming and ultrasonic; ≥7.67 mg/mL in DMSO |
Chemical Name | (2S)-N-[(2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(quinoline-2-carbonylamino)butanediamide;methanesulfonic acid |
SDF | Download SDF |
Canonical SMILES | CC(C)(C)NC(=O)C1CC2CCCCC2CN1CC(C(CC3=CC=CC=C3)NC(=O)C(CC(=O)N)NC(=O)C4=NC5=CC=CC=C5C=C4)O.CS(=O)(=O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
- 批次: