| 产品描述： | RS-102895 hydrochloride (HCl) 是一种有效的 Chemokine (C-C motif) receptor 2 (CCR2) 的拮抗剂，其IC50值为360 nM，对CCR1无影响。RS-102895 hydrochloride 还可抑制细胞中的 human α1a 和 α1d receptors，大鼠脑皮质 5-HT1a receptor，其IC50值分别为130 nM、320 nM和470 nM |
| 靶点： |
human α1a receptor(Cell-free assay):130 nM; human α1d receptor(Cell-free assay):320 nM; CCR2(Cell-free assay):360 nM; 5-HT1a receptor(Cell-free assay):470 nM;Others; 5-HTReceptor; CCR |
| 体外研究： |
An in vitro chemotaxis assay validates the effect of RS-102895 on leukocyte chemotaxis toward CCL2. The results suggest that increased CCL2 in SS kidneys is important in the early recruitment of leukocytes, and blockade of this recruitment by administering RS-102895 subsequently blunts the renal damage and hypertension |
| 体内研究： |
The functional role of the CCL2/CCR2 pathway is tested by daily administration of CCR2 antagonist RS-102895. Blood pressure, renal leukocyte infiltration, and renal damage are evaluated. The results demonstrates that RS-102895 treatment ameliorates renal damage and hypertension after 21 days of high-salt diet. It is determined that renal leukocyte infiltration is blunted by day 3 of the high-salt diet |
| 细胞实验： |
Cell lines: peritoneal cells Concentrations: 1 μM, 10 μM, 100 μM, 350 μM Incubation Time: 30 min Method: Peritoneal cells are collected and then passed through a 40-μm strainer, centrifuged, and resuspended in serum-free medium. Cells are then counted by hemocytometer, and the concentration was adjusted to 107 cells/mL. Cells are either untreated or incubated for 30 min with RS-102895 at varying concentrations, DMSO vehicle, or urine from in vivo CCR2 antagonist-treated animals. |
| 动物实验： |
Animal Models: 7-wk-old male Dahl SS rats Dosages: 5 mg/kg Administration: i.p. |
| 参考文献： |
1. T Mirzadegan, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71. 2. Ammar J Alsheikh, et al. CCL2 mediates early renal leukocyte infiltration during salt-sensitive hypertension. Am J Physiol Renal Physiol. 2020 Apr 1;318(4):F982-F993. |
| 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 |
2.343 ml |
11.713 ml |
23.427 ml |
| 5 mM |
0.469 ml |
2.343 ml |
4.685 ml |
| 10 mM |
0.234 ml |
1.171 ml |
2.343 ml |
| 50 mM |
0.047 ml |
0.234 ml |
0.469 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