human ccr1

BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist.

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with a Ki of 1 nM for human CCR1, exhibiting 250-fold selectivity over CCR2, CCR5, and CXCR4.

Met-RANTES (human) acetate is the acetate salt form of Met-RANTES (human). It acts as an antagonist for CCR1 and CCR5 receptors. This compound inhibits the human chemokines MIP-1α and MIP-1β, with respective IC50 values of 5 and 2 nM. Additionally, Met-RANTES (human) acetate reduces bone destruction and alleviates adjuvant-induced arthritis (AIA) in rats.

RS 504393 is a highly selective CCR2 chemokine receptor antagonist (IC50s: 89 nM and > 100 μM for human recombinant CCR2 and CCR1).

BAY-3153 is a selective CCR1 (C-C motif chemokine receptor 1) antagonist with an IC50 of 3 nM in humans, 11 nM in rats, and 81 nM in mice.

Cis-J-113863 is a competitive antagonist for the chemokine receptor 1 (CCR1), demonstrating inhibitory concentration 50 (IC50) values of 0.9 nM for human CCR1 receptors and 5.8 nM for mouse CCR1 receptors, respectively [1].

CCR1 antagonist12 (Compound 12) is an antagonist of CCR1, exhibiting an IC50 of 3 nM against human CCR1. It inhibits the chemotaxis through pores induced by CCL3, with an IC50 of 0.009 µM. Additionally, CCR1 antagonist12 demonstrates favorable pharmacokinetic properties in a rat model.

RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.