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CAS No.: 1173022-16-6

RS102895 HCl Catalog No. CSN13797

Synonyms: RS-102895 HCl;RS 102895 (hydrochloride);RS-102895

RS102895 HCl is a potent and specific CCR2 antagonist with binding IC50 of 360 nM, no significant inhibition on CCR1 (IC50 > 17 μM).

规格	价格	促销价格	库存	数量

400-920-2911

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CCR2

bindingIC50:360nM
描述Chemokine monocyte chemoattracant-1 (MCP-1) stimulates leukocyte chemotaxis to the inflammatory sites by binding to its receptor CCR2, which belongs to G-protein-coupled transmembrane receptor superfamily. RS-102895 hydrochloride is a spiropiperidine compound that acts as an antagonist of MCP-1 to block CCR2 binding with an IC50 value of 360 nM. An inhibition of MCP-1-induced calcium influx by RS-102895 hydrochloride was observed in CCR2-CHL cells with an IC50 value of 32 nM. RS-102895 hydrochloride also inhibited MCP-3-induced calcium influx with IC50 at 130 nM. When decidual stromal cells (DSCs) were treated with 1 ng/ml IL-33 and 100 ng/ml RS-102895 hydrochloride for 48 hours, the proliferation and invasiveness of DSCs were significantly decreased. When mice were dosed with RS-102895 hydrochloride every 6 hours at 5 mg/kg i.p. for a total of 4 treatments, the recruitment of inflammatory monocytes to vaccine draining lymph nodes was significantly reduced at both 12 and 24 hours post immunization. Also in mice immunized with 1 µg HA1, an influenza antigen, and boosted for 10 days, 5 consecutive treatments of 5 mg/kg RS102895 hydrochloride administered 6 hours apart by i.p. injection significantly increased interferon gamma responses and the production of anti-HA1 IgG.
作用机制RS-102895 hydrochloride prevents MCP-1 from binding to CCR2 by occupying the same binding-site, the inter-helical bundle region on the extracellular side of CCR2 receptor.
动物研究
剂量
Mice: 5 mg/kg^[3] (i.p.), 20 mg/kg^[4] (i.p.) Rat: 2 mg/kg^[5] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[3] (i.p.), 20 mg/kg^[4] (i.p.) Rat: 2 mg/kg^[5] (i.p.)
给药途径	i.p.

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
- 2.3427 mL
- 11.7134 mL
- 23.4269 mL
- 5 mM
- 0.4685 mL
- 2.3427 mL
- 4.6854 mL
- 10 mM
- 0.2343 mL
- 1.1713 mL
- 2.3427 mL

技术信息

CAS号

1173022-16-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H22ClF3N2O2

运输

蓝冰

分子量

426.86

别名

RS-102895 HCl;RS 102895 (hydrochloride);RS-102895

溶解度

DMSO	12.57 mg/mL (29.5 mM)
Water	insoluble

动物实验配方

5%DMSO+H2O

1 mg/mL

clear

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