BMS-663068
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.
BMS-663068是一种小分子HIV-1 gp120附着抑制剂[1]。
HIV-1病毒进入宿主细胞的第一步,是病毒gp120包膜糖肽结合到宿主细胞的CD4受体。BMS-663068是一种针对特定HIV-1分离株的附着抑制剂,并靶向这一步骤。BMS-663068是一种膦酰甲基前药,可以被肠道内的碱性磷酸酶裂解,然后释放有效部分BMS-626529。与祖先附着抑制剂BMS-488043相比,BMS-663068具有改善的抗病毒谱[1]。
BMS-663068在细胞培养物中显示低细胞毒性。在PM1和PBMC细胞中,CC50值分别为105和192 μM。在HEK293、HepG2、HCT116、HeLa、MT-2、MCF-7和H292细胞中,CC50值均大于200 μM。结果发现,BMS-663068对HIV的实验室菌株和临床分离株都具有强效的抗病毒活性。对CXCR4-tropic LAI病毒,BMS-663068的EC50值为0.7 nM。对包括NL4-3、SF-162和JRFL在内的实验室菌株,BMS-663068的抑制功效比BMS-488043的抑制功效高7至10倍。当用89.6病毒(15倍)、Bal病毒(14倍)和MN病毒(67倍)处理时,BMS-663068比BMS-488043的功效更强。在使用PBMC细胞抗病毒试验中,BMS-663068用于抑制获取自美国国立卫生研究院艾滋病库的共88种HIV-1病毒。BMS-663068针对最敏感病毒的EC50值为0.01 nM,针对最不敏感病毒的EC50值为2 μM。此外,对其他HIV-1进入抑制剂(如ENF和ibalizumab)耐药的病毒保留对BMS-626529的敏感性[1和2]。
参考文献:
[1] Nowicka-Sans B, Gong YF, McAuliffe B, Dicker I, Ho HT, Zhou N, Eggers B, Lin PF, Ray N, Wind-Rotolo M, Zhu L, Majumdar A, Stock D, Lataillade M, Hanna GJ, Matiskella JD, Ueda Y, Wang T, Kadow JF, Meanwell NA, Krystal M. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrob Agents Chemother. 2012 Jul;56(7):3498-507.
[2] Li Z, Zhou N, Sun Y, Ray N, Lataillade M, Hanna GJ, Krystal M. Activity of the HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068, against CD4-independent viruses and HIV-1 envelopes resistant to other entry inhibitors. Antimicrob Agents Chemother. 2013 Sep;57(9):4172-80.
Storage | Store at -20°C |
M.Wt | 583.49 |
Cas No. | 864953-29-7 |
Formula | C25H26N7O8P |
Synonyms | BMS663068;BMS 663068 |
Solubility | Soluble in DMSO |
Chemical Name | (3-(2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl)-4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-1-yl)methyl dihydrogen phosphate |
SDF | Download SDF |
Canonical SMILES | CC1=NN(C2=NC=C(OC)C3=C2N(COP(O)(O)=O)C=C3C(C(N4CCN(C(C5=CC=CC=C5)=O)CC4)=O)=O)C=N1 |
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。 |