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RS 504393

产品编号 T5384 CAS 300816-15-3

RS 504393 是一种高度选择性的 CCR2 趋化因子受体拮抗剂，作用于人重组 CCR2 和 CCR1 受体，IC50值分别为 89 nM 和大于 100 μM。

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RS 504393, CAS 300816-15-3

规格	价格/CNY	货期
1 mg	￥ 265	现货
5 mg	￥ 672	现货
10 mg	￥ 1,220	现货
25 mg	￥ 2,670	现货
50 mg	￥ 3,920	现货
100 mg	￥ 5,380	现货
1 mL * 10 mM (in DMSO)	￥ 739	现货

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存储 & 溶解度

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产品描述	RS 504393 is a highly selective CCR2 chemokine receptor antagonist (IC50s: 89 nM and > 100 μM for human recombinant CCR2 and CCR1).
靶点活性	CCR2:89 nM (cell free), α1A-adrenoceptor:72 nM (cell free)
体外活性	RS-504393 inhibit MCP-1-stimulated calcium influx into CCR2-CHL cells. The IC50 values are 35 nM [1]. CCR2 antagonist, RS 504393 treatment, suppressed allergen induced β-hexosaminidase release significantly. This inhibitory effect was partially reversed by supplementation of recombinant MCP-1 protein (100 pg/mL) [2].
体内活性	Whereas vehicle-treated mice developed clear signs of acute inflammation, RS 504393-treated mice failed to show clinical signs of immediate hypersensitivity. No effect was observed in naive animals. The degranulation of mast cells was significantly inhibited in RS 504393-treated mice but had no effect on naive mice [2]. Similar to the results obtained from CCR2-deficient mice, the treatment with RS-504393 significantly reduced renal pathology, especially the extensive interstitial fibrosis mediated by a decrease in type I collagen synthesis [3].
激酶实验	Briefly, binding was measured using membranes prepared from two cell lines, THP-1 and CCR2-CHL cells. Each competition assay was composed of cell membranes, 50 pM 125I-MCP, MCP buffer, protease inhibitors, and test compound. Equilibrium was achieved by incubation at 28?°C for 90 min. Membrane-bound 125I-MCP was collected by filtration through GF/B filters presoaked in polyethyleneimine and bovine serum albumin, followed by four rapid washes with approximately 0.5 ml of ice-cold buffer containing 0.5 M NaCl and 10 mM HEPES, pH 7.4. MCP buffer consists of 50 mMHEPES, pH 7.2, 1 mM CaCl2, 5 mMMgCl2, and 0.1% bovine serum albumin. Protease inhibitors include 0.1 mM phenylmethylsulfonyl fluoride, 1 μM leupeptin, and 0.35 mg/ml pepstatin. THP-1 cells are a human monocyte cell line that express both CCR1 and CCR2. CCR2-CHL cells are Chinese hamster lung cells that have been stably transformed with an expression vector bearing the human CCR2b receptor [1].
细胞实验	Briefly, cytosolic calcium influx was measured in CCR2-CHL cells loaded with the fluorescent dye Fura-2-AM. Quantitation of signal intensity used the integrated signal intensity for 82 s after the addition of chemokine and thus has units of M·s. Antagonism by various compounds of calcium influx was measured using an approximate ED50 dose of MCP-1 (3 nM) and an approximate ED25 dose for MCP-3 (5 nM). Chemotaxis was measured over 1 h using THP-1–5X cells in a 96-well Boyden chamber apparatus. Cell migration through the polycarbonate filter was quantified by fluorescent staining using propidium iodide in 0.1% Triton X-100. These assays typically gave stimulated to unstimulated migration of 6-fold, range 4–10-fold, using a maximally effective concentration of MCP-1. Chemotaxis antagonist measurements used 3 nM MCP-1 or RANTES; these concentrations are near the ED95 attractant concentration for MCP-1 and for RANTES as agonists. The data are expressed by normalization to the uninhibited migration caused by the agonist chemokine. The antagonist was present in both chambers of the Boyden apparatus [1].
动物实验	To evaluate the therapeutic effects of MCP-1/CCR2 signaling, either propagermanium (3 or 8 mg/kg orally once a day) or RS-504393 (2 mg/kg orally twice a day) was mandatorily injected into their mouths to wild-type mice from 3 days before ureteral ligation until the day of sacrifice. In addition, to determine the viability for the usage of CCR2 antagonists for the treatment of renal fibrosis, propagermanium (8 mg/kg) was given daily, beginning 4 days after ureter ligation. For pathological examination, both the obstructed and contralateral kidneys were harvested from UUO animals 4, 7, and 14 days after ureteral ligation (n = 5 at each time point). Untreated age-matched male wild-type mice and CCR2-deficient mice were used as normal control (n = 6 for each group). Since propagermanium treatment was started from 3 days before ureteral ligation, mice treated with propagermanium for 3 days at day 0 were used as a negative control (n = 5) [3].

分子量	417.5
分子式	C25H27N3O3
CAS No.	300816-15-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 10 mg/mL (23.95 mM)

H2O: Insoluble

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3952 mL	11.976 mL	23.9521 mL	59.8802 mL
	5 mM	0.479 mL	2.3952 mL	4.7904 mL	11.976 mL
	10 mM	0.2395 mL	1.1976 mL	2.3952 mL	5.988 mL
	20 mM	0.1198 mL	0.5988 mL	1.1976 mL	2.994 mL

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参考文献

1. Mirzadegan T, 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. Tominaga T, et al. Blocking mast cell-mediated type I hypersensitivity in experimental allergic conjunctivitis by monocyte chemoattractant protein-1/CCR2. Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5181-8. 3. Kitagawa K, et al. Blockade of CCR2 ameliorates progressive fibrosis in kidney. Am J Pathol. 2004 Jul;165(1):237-46.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

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% ddH₂O

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计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

RS 504393 300816-15-3 Immunology/Inflammation Microbiology/Virology CCR CC chemokine receptor RS504393 Inhibitor inhibit RS-504393 inhibitor

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RS 504393

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参考文献

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剂量换算

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