- 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.
Science.2016 Aug 5;353(6299)594-8
Nat Nanotechnol.2017 Dec;12(12):1190-1198.
Nature Biotechnology.2017 Jun;35(6):569-576
Nat Med.2018 Sep 17.
Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.
Cell.Available online 25 October 2018.
Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.
Cell.2018 Jun 28;174(1):172-186.e21.
Cell.2018 Feb 22;172(5):1007-1021.e17.
Cell.2017 Nov 30;171(6):1284-1300.e21.
Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.
Cell.2017 Jul 13;170(2):312-323
Nat Med.2018 Jan 29.
Nat Med.2017 Nov;23(11):1342-1351.
Cell.2017 Apr 6;169(2):286-300.
Cell.2015 Aug 27;162(5):987-1002.
Cell.2015 Feb 12;160(4):729-44.
Nature Medicine.2017 Apr;23(4):493-500.
Cancer Cell.2018 May 14;33(5):905-921.e5.
Cancer Cell.2018 Apr 9;33(4):752-769.e8.
Cancer Cell.2018 Mar 12;33(3):401-416.e8.
Cancer Cell.2017 Aug 14;32(2):253-267.e5.
Nat Methods.2018 Jul;15(7):523-526.
Cell Stem Cell.2018 May 3;22(5):769-778.e4.
Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure


BMS-663068 Dilution Calculator
calculate

BMS-663068 Molarity Calculator
calculate
| 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.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
>
靶向性——脂微球载体以其特有的亲和力聚集于病变部位;
持续性——在脂微球的保护作用下,前列地尔主要在肺部的灭活明显降低;
高效性——仅需传统剂型几十分之一的给药量,且疗效更佳;
低副作用——在脂微球的屏障作用下,前列地尔对血管的刺激和炎性反应明显减少;
“脂微球保护技术”的引入,使得优帝尔的剂型稳定性更高,用药更安全:
剂型稳定性更高——优帝尔仅需在阴凉处(不超过20℃)保存,这样带来的好处是:南方地区无需冷藏储存,北方地区也不用再担心药物因温度过低而冻结,从而影响临床用药。(蓓畅、凯时等同类产品在运输、贮藏过程中必须保证环境温度范围在0-5℃)
用药更安全——市场上已有北京泰德制药有限公司生产的“前列地尔注射液”,商品名“凯时”,该品种也是运用脂微球化技术的一类制剂。但是该品种由于自身生产工艺的缺点,其中的主要杂质—PGA1相当高,质量标准中规定其限度高达60%,对产品中其他杂质也未进行控制。而药友公司通过长达近10年的摸索,通过无菌过滤和低温冷冻干燥技术,制备的“注射用前列地尔干乳剂”可将杂质PGA1严格控制在10%以内,其他杂质控制在1%以内,表明药友公司采用的冷冻干燥方法更加有利于产品的质量控制。因此药友公司注射用前列地尔干乳剂提出了比“凯时”更为严格的质量标准要求,有效保证产品质量。由于本品质量的提升,使得本品可以储存在常见的阴凉条件下,而不是“凯时”相当苛刻的储存条件要求。药友公司技术人员通过大量科学研究,探索出特殊的冻干保护剂和严格的冻干过程控制实现了脂微球的冻干技术,使本品既保留了脂微球的物理性质,又显著提升了脂微球的化学稳定性。因此,“优帝尔”的执行标准仅为前列地尔注射液执行标准的六分之一。
以FITC和PE为例来看光谱重叠。FITC单染管的荧光会部分漏到PE通道中,而这部分需要从PE通道中减掉溢漏过来的FITC荧光。那么荧光补偿该如何调节呢?l 调节电压l 检测荧光通道的自发荧光l 每个荧光通道做单染管对照检测何为单染管对照?l 细胞l 补偿微球细胞通常是流式抗体单染管对照的样本首选,但是当细胞数量有限,无多余细胞用于抗体单染或感兴趣的表面抗原表达较低,阳性分群不明显不足以用来调节补偿时,建议选择补偿微球。补偿调节时要注意:l 使用未染色的细胞做PMT的电压设置l 不要使用未染色的补偿微球设置电压eBioscience提供两种补偿微球:OneComp eBeads与UltraComp eBeads。微球大小和淋巴细胞相当,可连接各种荧光标记的抗体来调节补偿。每滴微球中都含有两群:一群是可以结合抗体的阳性群,一群是不会与抗体反应的阴性群。优点:l 使用方便,一滴即可l 使用实验抗体与微球有效结合调节补偿,无需再用CD4分群来调节l 细胞替代物,适应各种孵育时间,结果稳定流式细胞术中荧光补偿该如何调节?l 能与各种种属和亚型的抗体反应ProductSpecies CompatibilityChain RecognitionFeaturesMouse IgRat IgHamster IgRabbit IgKappa Light ChainLambda Light ChainOne DropOne VialAll cell sizesViolet LaserUltraComp eBeads 01-2222√√√√※√√√√√√OneComp eBeads 01-1111√√√√※√√√√√Competitor X Anti-Mouse Ig, k√√Competitor X Anti-Rat Ig, k√√Competitor X Anti-Rat/Hamster Ig, k√√√Competitor X Plus Anti-Mouse Ig, k√√Competitor X Plus Anti-Rat Ig, k√√Competitor Z Anti-Mouse Bead Kit√√√
竞争品牌的微球是分种属的,使用不同抗体要购买多个产品以使用注:兔来源的抗体与微球结合力较弱,但某些还是可以使用l 适用于各种激发光---适用于488 nm 蓝光,532 nm 绿光,561 nm 黄光,633-635 nm 红光,UltraComp eBeads尤其适用紫外 (355 nm) 或者 紫色 (405 nm) 激光器l 微球本身信号经过优化适合补偿调节l 价格相当,有小包装操作步骤:1. 准备好流式管,每种荧光抗体一个;2. 将微球翻转或者涡旋混匀;3. 在每管中加入一滴微球;4. 在管中分别加入相应的 1 test 抗体(不同抗体 1 test 的用量不同,具体参见说明书);5. 敲击或者涡旋混匀;6. 2-8℃暗处孵育 15-30 分钟;7. 每管加 2ml 流式染色缓冲液,400-600 x g 离心 3-5 分钟;8. 弃上清,每管加入 0.2-0.4 mL 流式染色缓冲液;9. 混匀后上机分析
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。
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.

