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RS102895

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Chemical Structure| 300815-41-2 同义名 : -
CAS号 : 300815-41-2
货号 : A642498
分子式 : C21H21F3N2O2
纯度 : 99%
分子量 : 390.399
MDL号 : MFCD08703093
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(640.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 45 mg/mL(115.27 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.81mL

2.56mL

1.28mL

25.61mL

5.12mL

2.56mL
参考文献

[1]Mirzadegan T, Diehl F, 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;275(33):25562-71.

[2]Hu WT, Li MQ, et al. IL-33 enhances proliferation and invasiveness of decidual stromal cells by up-regulation of CCL2/CCR2 via NF-κB and ERK1/2 signaling. Mol Hum Reprod. 2014;20(4):358-72.

[3]Mitchell LA, Hansen RJ, et al. Optimized dosing of a CCR2 antagonist for amplification of vaccine immunity. Int Immunopharmacol. 2013;15(2):357-63.