| 产品描述： | BX471 (ZK811752, BAY 865047, SH T 04268H) 是一种有效的非肽 CC 趋化因子受体-1 (CCR1) 拮抗剂，在 MIP-1α 和 MCP-3 与 CCR1 转染的 HEK23 细胞结合中，Ki 值分别为 1 nM 和 5.5 nM |
| 靶点： |
CCR1(in MIP-1α binding assay):1 nM(ki); CCR1(in MCP-3 binding assay):5.5 nM(ki);CCR |
| 体外研究： |
By displacing the ligand binding to CC chemokine receptor-1 (CCR1), BX 471, a potent antagonist, can inhibit the effects medicated by CCR1. In addition, BX-471 exhibits anti-allergic effect by increasing Treg cell population |
| 体内研究： |
For fasted dogs, the half-life for BX 471 was approximately 3 h, with an oral bioavailability of approximately 60%. In rats of EAE model, CCR1 antagonist, BX 471, dose-dependently decreased the severity of the disease |
| 细胞实验： |
Cell lines: THP-1- or CCR1-transfected HEK293 cells Concentrations: 10 µM Incubation Time: 24 h Method: Binding assays were performed by filtration. Radiolabeled chemokines at a final concentration of approximately 0.1–0.2 nM were used as ligand. HEK293 cells expressing human CCR1 at 8,000 or 300,000 cells per assay point were used as the receptor source. Nonspecific binding was determined in the presence of 100 nM unlabeled chemokine. The binding data were curve-fitted with the computer program IGOR (Wavemetrics) to determine the affinity and number of sites. To demonstrate that CCR1 antagonism by BX 471 was not due to the cellular toxicity of the compound, THP-1- or CCR1-transfected HEK293 cells were treated with BX 471 at concentrations up to 10 µM for 24 h, and cellular toxicity was monitored by measuring WST-1 staining. No significant toxicity was observed |
| 动物实验： |
Animal Models: Fasted male beagle dogs; Male Lewis Rats of EAE model Dosages: 4 mg/kg (for fasted male beagle dogs); 20 and 50 mg/kg (for Male Lewis Rats) Administration: p.o. |
| 参考文献： |
1. M Liang, et al. 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. 2. Feng S, et al. Therapeutic Effect of C-C Chemokine Receptor Type 1 (CCR1) Antagonist BX471 on Allergic Rhinitis. J Inflamm Res. 2020 Jul 21;13:343-356. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.299 ml |
11.497 ml |
22.994 ml |
| 5 mM |
0.46 ml |
2.299 ml |
4.599 ml |
| 10 mM |
0.23 ml |
1.15 ml |
2.299 ml |
| 50 mM |
0.046 ml |
0.23 ml |
0.46 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京