Drug intelligence / Profile preview

RS102895

Development stage
Preclinical
Modality
Classical Binding Small Molecules → Small Molecules
01

Overview

RS102895 is a small molecule chemokine receptor antagonist that selectively targets the C-C chemokine receptor type 2 (CCR2), particularly the CCR2b isoform. It belongs to the spiropiperidine structural class and exhibits high potency and selectivity for CCR2b over other related receptors such as CCR1. The compound inhibits monocyte chemoattractant protein-1 (MCP-1/CCL2)-induced calcium influx and chemotaxis in vitro, with reported IC50 values of approximately 360 nM for CCR2 inhibition and much weaker activity against CCR1. RS102895 has been widely used as a research tool to study inflammation, immune cell trafficking, renal injury, cancer biology, and neuroinflammation in preclinical models[1][3][5]. It is not approved for clinical use but is active in vivo in animal studies[7]. The drug has also been referred to as "Abaucin" in some literature[9].

Other names
RS 102895 hydrochlorideRS102895 hydrochlorideRS-102895 hydrochlorideAbaucinMLJS-21001MLJS21001MLJS 21001
02

Targets

CCR2B (C-C chemokine receptor type 2B)ADRA1D (α1D)ADRA1A (α1A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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