300816-15-3|RS-504393|CsnPharm

CAS No.: 300816-15-3

RS 504393 Catalog No. CSN12845

Synonyms: Rs-504393

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述RS-504393 is a selective CCR2 antagonist with Kd value of 105nM. It inhibited MCP-1 binding measured in THP-1 with IC50 value of 89nM. RS-504393 at concentration ranging in 0.1-10μM dose-dependently inhibited chemotaxis of THP-1 cells driven by MCP-1 (3nM). RS-504393 blocked cytosolic calcium influx into CCR2-CHL cells caused by MCP-1 (3nM) or MCP-3 (5nM) with IC50 value of 35nM and 160nM, respectively. Subcutaneous injection of RS504393 at dose of 1mg/kg to mice at 24 and 0.5 h prior to EtOH exposure significantly reduced ethanol-induced microglia activation/neuroinflammation, and neuroapoptosis in the developing brain.
作用机制RS-504393 prevent MCP-1 binding by occupying the inter-helical bundle region on the extracellular side of the receptor.
参考文献

[1] Baamonde A, Hidalgo A, et al. Involvement of glutamate NMDA and AMPA receptors, glial cells and IL-1β in the spinal hyperalgesia evoked by the chemokine CCL2 in mice. Neurosci Lett. 2011 Sep 20;502(3):178-81.
[2] Yang D, Tong L, et al. Roles of CC chemokine receptors(CCRs) on lipopolysaccharide-induced acute lung injury. Respir Physiol Neurobiol. 2010 Mar 31;170(3):253-9.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3952 mL
- 11.9760 mL
- 23.9521 mL
- 5 mM
- 0.4790 mL
- 2.3952 mL
- 4.7904 mL
- 10 mM
- 0.2395 mL
- 1.1976 mL
- 2.3952 mL

技术信息

CAS号

300816-15-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H27N3O3

运输

蓝冰

分子量

417.50

别名

Rs-504393

溶解度

DMSO	12.0 mg/mL (28.7 mM) warming
Water	Insoluble

动物实验配方

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