| BMS-378806Gp120/CD4 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Description | BMS-378806 is a selective inhibitor of HIV-1 CD4-gp120 interactions with an EC50 value of 0.85-26.5 nM. | |||||
| Targets | CD4-gp120 interactions | |||||
| IC50 | 0.85 nM-26.5 nM(EC50) | |||||
| Kinase experiment [1]: | |
Drug susceptibility Assay | In general, host cells are infected with HIV-1 at a multiplicity of infection (MOI) of 0.005 50% tissue culture infective doses (TCID50)/cell followed by incubation in the presence of serially diluted inhibitors for 4 to 7 days. Virus yields are quantitated using an RT assay or a p24 enzyme-linked immunosorbent assay (ELISA) (NEN). The results from at least three experiments are used to calculate the 50% effective concentrations (EC50s). The EC50s of IDV, SQV, RTV, and NFV are compared to that of BMS-806 using Dunnett"s test. These comparisons are made separately within each assay system. Dunnett"s test is used to reduce the probability of false-positive results when a number of treatments are being compared to a control. Confidence bounds for the fold increases in EC50s observes when the same drug is tested in two different assay systems are computed using Fieller"s theorem. The use of this theorem is necessary because ratios of parameters (in this case, EC50s) are known not to follow a standard probability distribution, such as the normal distribution. Numbers within the confidence interval are not significantly different from the observed fold increase at the 95% level. |
| Cell experiment: | |
Cell lines | MT-2 cells |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 0-3 mM for 6 days; or 0.8, 1.6, and 3.2 μM |
Applications | BMS-378806 showed HIV-1 inhibitory activity and cytotoxicity in MT-2 cells with EC50 value of 2.68 nM [1]. Moreover, BMS-378806 inhibited the interaction between viral gp120 and cellular CD4 receptors and showed direct binding affinity to gp120 [2]. |
| Animal experiment: | |
Animal models | Rats, monkeys and dogs model. |
Dosage form | i.v. 1 and 5 mg/kg and p.o. 5 and 25 mg/kg for 0.17, 0.5, 1, 1.5 and 2 h |
Applications | BMS-378806 showed species-dependent oral bioavailability which was 19%–24% in rats and monkeys and 77% in dogs [3]. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: 1. Wang, T., Zhang, Z., Wallace, O. B., Deshpande, M., Fang, H., Yang, Z., Zadjura, L. M., Tweedie, D. L., Huang, S., Zhao, F., Ranadive, S., Robinson, B. S., Gong, Y. F., Ricarrdi, K., Spicer, T. P., Deminie, C., Rose, R., Wang, H. G., Blair, W. S., Shi, P. Y., Lin, P. F., Colonno, R. J. and Meanwell, N. A. (2003) Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. J Med Chem. 46, 4236-4239 2. Guo, Q., Ho, H. T., Dicker, I., Fan, L., Zhou, N., Friborg, J., Wang, T., McAuliffe, B. V., Wang, H. G., Rose, R. E., Fang, H., Scarnati, H. T., Langley, D. R., Meanwell, N. A., Abraham, R., Colonno, R. J. and Lin, P. F. (2003) Biochemical and genetic characterizations of a novel human immunodeficiency virus type 1 inhibitor that blocks gp120-CD4 interactions. J Virol. 77, 10528-10536 3. Yang, Z., Zadjura, L., D"Arienzo, C., Marino, A., Santone, K., Klunk, L., Greene, D., Lin, P. F., Colonno, R., Wang, T., Meanwell, N. and Hansel, S. (2005) Preclinical pharmacokinetics of a novel HIV-1 attachment inhibitor BMS-378806 and prediction of its human pharmacokinetics. Biopharm Drug Dispos. 26, 387-402 | |
BMS-378806 Dilution Calculator
calculate
BMS-378806 Molarity Calculator
calculate
| Cas No. | 357263-13-9 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 1-[(2R)-4-benzoyl-2-methylpiperazin-1-yl]-2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethane-1,2-dione | ||
| Canonical SMILES | CC1CN(CCN1C(=O)C(=O)C2=CNC3=NC=CC(=C23)OC)C(=O)C4=CC=CC=C4 | ||
| Formula | C22H22N4O4 | M.Wt | 406.43 |
| Solubility | ≥20.2mg/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. | ||
BMS-378806 is a novel attachment inhibitor of HIV with EC50 values of 2.68±1.64nM, 26.5±3.5nM, 2.94±2.01nM,15.5±6.8nM, 3.46±0.81nM, 1.47±0.63nM and 0.85±0.13nM for LAI(T), SF-2(T),NL4-3(T), Bal(M), SF-162(M), JRFL(M) and TLAV(dual), respectively [1].
In a series of in vitro biochemical assay, BMS-378806 has been found to be not an effective inhibitor of HIV integrase, protease, or reverse transcriptase, but compete with soluble CD4 binding to a monomeric form of gp120 protein in an ELISA assay with an IC50 value of ~100nM. In addition, BMS-378806 has shown no overt cytotoxicity toward the host cell with a CC50 value of >225μM [1].
References:[1] Wang T1, Zhang Z, Wallace OB, Deshpande M, Fang H, Yang Z, Zadjura LM, Tweedie DL, Huang S, Zhao F, Ranadive S, Robinson BS, Gong YF, Ricarrdi K, Spicer TP, Deminie C, Rose R, Wang HG, Blair WS, Shi PY, Lin PF, Colonno RJ, Meanwell NA. Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. J Med Chem. 2003 Sep 25;46(20):4236-9.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
>
我的邮箱：maoyuanqing@citiz.net
**捷向您推荐美国Trevigen的一款通用PARP分析试剂盒检测试剂盒。该试剂盒是检测凋亡前与凋亡中细胞提取液中PARP活性的理想方案，操作简单，重复性高。其通过检测96孔板上生物素标记的多聚ADP核糖聚合到邻近组蛋白的反应，从而确定已知的或可能的PARP抑制剂。试剂盒中的依托泊苷（Etoposide）是拓扑异构酶Ⅱ抑制剂，在拓扑异构酶Ⅱ切割完DNA后能够稳定该酶。在试剂盒中，依托泊苷作为凋亡诱导的对照参与检测。
通量PARP/凋亡分析试剂盒可广泛应用于1）检测原代、肿瘤等细胞的PARP活性；2）检测凋亡前后的PARP活性；3）利用细胞裂解液筛选PARP抑制剂。
试剂盒特色比色法/化学发光法，无放射性输出。96well，高通量检测。极大地节省了分析时间，提高了使用效率。高敏感性。能够检测到500个细胞中低至0.1mU的PARP。检测范围广。0.1-10mU。样本用量少。仅仅需要10-100ng的提取物。检测时间短。仅需要3h即可完成检测。
**捷向您提供一站式的PARP相关实验解决方案，除了高通量PARP/凋亡分析试剂盒，还有PARP体内药理动力学二代分析试剂盒(PDAII)和通用PAPR分析试剂盒外(含组蛋白包被可拆卸板)，以及相关抗体和重组蛋白。
Trevigen是一家快速成长的美国生物技术公司，专注于细胞凋亡、DNA损伤和修复、肿瘤细胞功能与行为等方面研究的肿瘤研究产品和服务。作为Trevigen在中国区域的总代理，**捷与Trevigen一道为中国的科研工作者提供最好、最新的氧化应激、细胞损伤和肿瘤细胞行为研究等领域内的优质产品和技术服务。如果您对上述产品及方案感兴趣，请致电400-6800-868至**捷科技有限公司垂询血管生成研究的相关实验解决方案，或索取最新的产品资料。
A.优点：
多重分析——一次分析可以检测16种干细胞相关的TF
定量比较——二个样本的差异可以定量分析和比较
步骤简单——探针温育、柱分离、板杂交和HRP检测
无需贵重仪器——无需如Luminex那样的贵重仪器
B.原理：
干细胞转录因子活性多重检测阵列试剂用于同时检测多种TF活性。该技术中，基于TFDNA结合位点的一致性序列，制备一系列生物素标记的探针。当探针混合物与核提取物一起温育时，每个探针寻找相应的TF，形成TF/探针复合物，通过柱离心纯化可以很容易与游离探针分开。结合的探针从混合物中分离出来，通过板杂交分析。板孔中预包被上与探针互补的特异序列，捕获的DNA探针进一步用链酶亲和素-HRP检测，化学发光检测仪测定发光强度（RLUs）。
