BX 471
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.
Ki:1 nM至5.5 nM
趋化因子受体1(CCR1)是用于治疗自身免疫疾病的主要治疗靶标.BX 471是CCR1的有效的选择性拮抗剂,具有口服活性.
体外实验:竞争结合研究表明,BX 471能够高亲和力置换CCR1配体,即巨噬细胞炎性蛋白1α\RANTES和单核细胞趋化蛋白-3.BX 471能够抑制大量CCR1介导的作用,是有效的功能性拮抗剂.与28种G-蛋白偶联受体相比,BX 471对CCR1具有大于10,000倍的选择性[1].
在体实验:药代动力学研究表明,在狗中,BX 471具有口服活性,有60％的生物利用度.此外,在多发性硬化症的大鼠实验性变应性脑脊髓炎模型中,BX 471有效地减少疾病[1].
临床试验:到目前为止,BX 471仍处于临床前开发阶段.
参考文献：
[1] Liang M, Mallari C, Rosser M, Ng HP, May K, Monahan S, Bauman JG, Islam I, Ghannam A, Buckman B, Shaw K, Wei GP, Xu W, Zhao Z, Ho E, Shen J, Oanh H, Subramanyam B, Vergona R, Taub D, Dunning L, Harvey S, Snider RM, Hesselgesser J, Morrissey MM, Perez HD. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 434.89 |
| Cas No. | 217645-70-0 |
| Formula | C21H24ClFN4O3 |
| Solubility | insoluble in H2O; ≥136.8 mg/mL in DMSO; ≥26.9 mg/mL in EtOH |
| Chemical Name | (R)-1-(5-chloro-2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)phenyl)urea |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC=C(C(NC(N)=O)=C1)OCC(N2[C@H](C)CN(CC(C=C3)=CC=C3F)CC2)=O |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
