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CAS No.: 300815-41-2

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

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400-920-2911

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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 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 was observed in CCR2-CHL cells with an IC50 value of 32 nM. RS-102895 also inhibited MCP-3-induced calcium influx with IC50 at 130 nM^[1]. When decidual stromal cells (DSCs) were treated with 1 ng/mL IL-33 and 100 ng/mL RS-102895 for 48 hours, the proliferation and invasiveness of DSCs were significantly decreased^[2]. When mice were dosed with RS-102895 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 administered 6 hours apart by i.p. injection significantly increased interferon gamma responses and the production of anti-HA1 IgG^[3].
作用机制RS-102895 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^[1].
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CAS号	300815-41-2	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C21H21F3N2O2	运输	蓝冰
分子量	390.40	别名

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