TMC353121
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.
TMC353121是一种呼吸道合胞病毒融合抑制剂.它是利用分子模拟方法,从前体分子JNJ-2408068中研制出来的.它维持高活性(pEC50 9.9)和低细胞毒性,而在肺部的保留时间较短(肺中的 t1/2为25小时).
研究发现,TMC353121通过阻止病毒细胞融合来抑制呼吸道合胞病毒,以及通过局部干扰呼吸道合胞病毒F蛋白的天然六股螺旋束结构来抑制合胞体的形成.
TMC353121减少治疗性和预防性给药的病毒载量.在BALB/c 小鼠模型中,TMC353121具有强效的抗病毒性能,保护其免受肺部感染和病毒诱发的炎症[2].
TMC353121具有剂量依耐性的抗病毒活性,其从峰值病毒载量的1log10减少到完全抑制呼吸道合胞病毒的复制不等.TMC353121 (0.39 μg/mL)完全抑制呼吸道合胞病毒脱落.与INFγ\IL6 及MIP1α剂量依耐性的减少相关.通常TMC353121作为CI给药16天耐受性良好[3].
参考文献：
1. Bonfanti JF, Meyer C, Doublet F et al. Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121). J Med Chem. 2008; 51: 875–896.
2. Olszewska W1, Ispas G, Schnoeller C et al. Antiviral and lung protective activity of a novel respiratory syncytial virus fusion inhibitor in a mouse model. Eur Respir J. 2011 Aug;38(2):401-8.
3. Ispas G, Koul A, Verbeeck J et al. Antiviral Activity of TMC353121, a Respiratory Syncytial Virus (RSV) Fusion Inhibitor, in a Non-Human Primate Model. PLoS One. 2015 May 26;10(5):e0126959.
| Storage | Store at -20°C |
| M.Wt | 558.71 |
| Cas No. | 857066-90-1 |
| Formula | C32H42N6O3 |
| Synonyms | TMC 353121; TMC-353121 |
| Solubility | Soluble in DMSO |
| Chemical Name | 2-[[6-[[2-(3-hydroxypropyl)-5-methylanilino]methyl]-2-(3-morpholin-4-ylpropylamino)benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=C(C=C1)CCCO)NCC2=CC3=C(C=C2)N=C(N3CC4=C(C=CC(=N4)C)O)NCCCN5CCOCC5 |
| 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。 |
| Description | TMC353121是一种强效的呼吸道合胞病毒(RSV)融合抑制剂,pEC50值为9.9. | |||||
| 靶点 | RSV | |||||
| IC50 | 9.9 (pEC50) | |||||
化学结构
