- NBD-556
- BMS-378806
| BMS-663068HIV-1 attachment inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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| Cas No. | 864953-29-7 | SDF | Download SDF |
| Synonyms | BMS663068;BMS 663068 | ||
| 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 | ||
| 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 | ||
| Formula | C25H26N7O8P | M.Wt | 583.49 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| 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. | ||
BMS-663068 is a small-molecule attachment inhibitor of HIV-1 gp120 with IC50 value of [1].The first step of HIV-1 virus to entry host cells is the binding of the viral gp120 envelope glycopeptide to the CD4 receptor of host cell. BMS-663068 is an attachment inhibitor against specific HIV-1 isolates and targets this step. It is a phosphonooxy methyl prodrug and can be cleaved by alkaline phosphatase in the gut then releases the effective moiety BMS-626529. Compared with the progenitor attachment inhibitorBMS-488043, BMS-663068 has an improved antivirus spectrum [1]. BMS-663068 showed low cytotoxicity in cell culture. In PM1 and PBMC cells, the CC50 values were 105 and 192 μM, respectively. In HEK293, HepG2, HCT116, HeLa, MT-2, MCF-7 and H292 cells, the CC50 values were all higher than 200 μM. It was found that BMS-663068 has potent anti-virus activity against both the laboratory strains and the clinical isolates of HIV. For the CXCR4-tropic LAI virus, BMS-663068 showed EC50 value of 0.7 nM. For a cohort of laboratory strains including NL4-3, SF-162 and JRFL, the inhibition efficacies of BMS-663068 against them were 7 to 10-fold higher than that of BMS-488043. It was even more potent than BMS-488043 when treated with 89.6 viruses (15-fold), Bal virus (14-fold) and MN virus (67-fold). In an antiviral assay using PBMC cells, BMS-663068 was treated against a total of 88 HIV-1 viruses obtained from the NIH AIDS Repository. It exerted an EC50 value of 0.01 nM against the most susceptible virus and an EC50 value of 2μM against the least susceptible virus. In addition, it was found that the virus resistant to other HIV-1 entry inhibitors such as ENF and ibalizumab retained susceptibility to BMS-626529 [1 and 2].References:[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.
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以BD出品的为例，你可以购买现成的或者可以根据你要检测的不同细胞因子和厂家定制bead array。基本原理就是试剂盒含有多种微球，每一种都是两种不同荧光强度组合，所以在流式检测的时候会形成一个矩阵。每种微球上附着有可以识别一种细胞因子的抗体。和样本孵育后，再加入荧光标记的抗不同细胞因子的抗体（同样颜色）。这样，只要微球上结合有细胞因子，这个微球就会有三种荧光了。
前两种荧光来判断是哪种微球（哪种细胞因子），第三种荧光是识别抗体上的，来定量。试剂盒还会提供标准品，用来做标准曲线。
细胞内的蛋白，用荧光标记的单克隆抗体识别后，用流式可以测出每个细胞的相对荧光强度。有一种特异性的微球，可以吸附一系列不同定量分子数的抗体。这种微球吸附同样的荧光抗体，可以做出荧光强度和所吸附抗体分子数量的标准曲线。然后拿细胞检测的荧光强度和这个标准曲线对比，得到细胞内所结合的抗体数。因为单克隆抗体只结合相同的抗原表位，所以可以推算出细胞内蛋白的分子数量了。
解释结果的时候要考虑到抗体的特异性和染色的效果等影响因素。
目前国内的制药企业对微粒释放系统的立项开发越来越多，园子里已经就脂质体展开了很多火热的讨论，我个人也参与其中，大家交流经验，取长补短，渐渐的找到了方向，系统而固定的讨论交流是非常有好处的。
因此在此倡议建立一个微球的交流区，让大家相互交流比如：微球产业化、技术难点、实验中遇到的问题、相关理论的探讨、最新进展交流等等
现分享于此：
LatexBeadsPhagocytosisassay
---Materials
*Fluorescencelabeledlatexbeads(1umdiameter),2.5%aqueoussUSPension
*3%BSAcontaining25mMNa2HPO4,pH6.0
*0,3%(w/v)azide
*Culturemediumcontaining5%FBS
*Distilledwater,PBS
*Bathsonication,6(12)-wellplates
---Cellcultureandtreatment
1,Inoculateplateswith7,0104cells/cm2perwell.Incubateat37℃,5%CO2for24hr,bestuntil50-70%confluenceisreached
2,Removeculturemediumandexposethecellstotestmaterial.Incubateat37℃,5%CO2for24hr.
---Preparationofcoatedlatexbeads
1，Washlatexbeadswithdistilledwaterandpelletat10,000gfor8minatRT.
2，Resuspendlatexbeadsin3%BSAcontaining25mMNa3PO4(pH6.0)andincubateatRTfor15minwithbathsonication.
*CoatingbeadsinBSAinsuresbeadsremaininamonodispersestate.
3，Washthebeadsoncewithculturemediumcontaining5%FBS.
4，Resuspendthebeadsinculturemediumatconcentration2.0%.Thisisbeadsstock.Storedindarknessat4℃.
---Assay
1，Controlsandsamples:Intactcontrol(Nostaining)1well
-Negativecontrol(azidetreated)1well
-Normalcontrol1well
-sample5wells
*Inordertodifferentiatebetweenphagocytosedbeadsandbeadsnonspecificallyadheretothecellsurface,controlcellsareexposedto0,3%(w/v)azidefor10minpriortotheadditionofcoatedbeads.Thistreatmentcompromisesmicroglialenergeticprocessesandfewbeadswereinternalizedasobservedbyfluorescentmicroscopy.Meanfluorescenceofazide-treatedmicrogliawasusedasthenegativecontrolandwassubtractedfromvaluesobtainedinexperimentalsamples.
2，Forexperimentsusing6well-plates,15μlbeadsstockin1mlculturemediumisappliedtoeachwell.Votexthebeadsstockwellandtakeout105μlandaddinto7mlculturemedium.Bathsonificatefor10minatRTindarkness.Thisisbeadsworkingsolution.
Forexperimentsusing12well-plates,6μlbeadsstockin0.4mlculturemediumisappliedtoeachwell.
3，WasheachwelltwicewithPBSandreplacewithbeadsworkingsolution,1ml/wellfor6-wellplate,0.4ml/wellfor12well-plate.Incubateinthedarkat37℃for80-120min.
4，Removebeadsworkingsolutionandwash3timeswithPBStoremoveexcessbeads.
5，LiftthecellsbyscrappingortrypsinizationandwashthecellswishPBS.
6，StainwithPI(4ug/mlfinalconcentration)andrunforFACS.
对于六分之一效率（99.9999％）ULPA过滤器，该系统挑战将产生100个粒子/ 立方英尺的下游气溶胶浓度或将在标称1.0cfm激光粒子计数器（LPC）中产生100个粒子/分钟的计数速率。
过滤器效率以及过滤器中任何相关联的泄漏可以通过LPC简单地检测。标准集团的高输出PSL气溶胶发生器取代了传统过滤器测试和无尘室认证中使用的DOP（邻苯二甲酸二辛酯）和其他油基气溶胶发生器。
