CCR2 Antagonist

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC₅₀ values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC₅₀ values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a K_i of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC₅₀ and EC₉₀ of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.

RS102895 is a potent CCR2 antagonist, with an IC₅₀ of 360 nM, and shows no effect on CCR1.

Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.

SD-24 is a selective antagonist targeting CCR2 with a K_i of 1 nM, and exhibits significantly reduced binding affinity to CXCR1 and CCR6. SD-24 is applicable for inflammation and immune-related research.

PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC₅₀s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.

RS102895 hydrochloride is a potent CCR2 antagonist, with an IC₅₀ of 360 nM, and shows no effect on CCR1.

BMS-813160 is a potent and selective CCR2/5 dual antagonist. BMS-813160 binds with CCR2 and CCR5 with IC₅₀s of 6.2 and 3.6 nM, respectively. BMS-813160 can be used for the research of inflammation.

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC₅₀s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC₅₀ of 24 nM.

Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.

YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the K_i values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.

CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC₅₀ of 103 nM.

INCB 3284 is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC₅₀ of 3.7 nM. INCB 3284 can be used in the research of acute liver failure.

CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC₅₀s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC₅₀ of 24 nM.

BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC₅₀ of 5.1 nM) and potent functional antagonism (calcium flux IC₅₀ of 18 nM and chemotaxis IC₅₀ of 1 nM).

MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2.

MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2.

AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC₅₀ of 1.2 nM for CCR2 Ca²⁺ flux .

CCR2 antagonist 3 is a chemokine receptor 2 (CCR2) antagonist.