ccr2 antagonist 1

CCR2 antagonist 1 is a high-affinity antagonist of CCR2 with a Ki of 2.4 nM and a long residence time.

(1S)-CCR2 antagonist 1, a left-handed chiral form of CCR2 antagonist 1, exhibits high affinity and a long residence time as a CCR2 antagonist, with an inhibition constant (K i) of 2.4 nM [1].

INCB 3284 is an orally available, selective and high affinity chemokine receptor 2 (CCR2) antagonist that inhibits monocyte chemotactic protein 1 from interacting with hCCR2.INCB 3284 is used in the study of hemorrhagic shock.

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

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

Cenicriviroc (TAK-652) is an orally active, dual CCR2 CCR5 antagonist that inhibits both HIV-1 and HIV-2, exhibiting potent anti-infective and anti-inflammatory activity.

Cenicriviroc Mesylate is a dual CCR2 CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist with IC50 values of 180 nM and 24 nM for CCR2 inhibition and MCP-1-induced chemotaxis inhibition, respectively.

BMS CCR2 22 is a potent and selective antagonist of CCR2 with calcium flux IC50 of 18 nM, chemotaxis IC50 of 1 nM, and binding IC50 of 5.1 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.

CCR2 antagonist 4 hydrochloride is a specific CCR2 antagonist (IC50s: 180 nM for CCR2b). It potently inhibits MCP-1-induced chemotaxis (IC50: 24 nM).

Emestrin, a mycotoxin originally isolated from *E. striata*, exhibits antimicrobial, immunomodulatory, and cytotoxic activities. It is effective against fungi *C. albicans* and *C. neoformans*, and bacteria *E. coli*, *S. aureus*, and methicillin-resistant *S. aureus* (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg ml, respectively). Emestrin acts as a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes). At 0.1 μg ml, it induces apoptosis in HL-60 cells and causes necrosis in heart, thymus, and liver tissues in mice at doses of 18-30 mg kg.