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• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *