Signaling Pathway

CCR

CCR

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CCR (Chemokine receptors) are cytokine receptors found on the surface of certain cells that interact with a type of cytokine called achemokine. There have been 19 distinct chemokine receptors described in mammals. Each has a 7-transmembrane (7TM) structure and couples to G-protein for signal transduction within a cell, making them members of a large protein family of G protein-coupled receptors. Following interaction with their specific chemokine ligands, chemokine receptors trigger a flux in intracellular calcium (Ca2+) ions (calcium signaling). This causes cell responses, including the onset of a process known as chemotaxis that traffics the cell to a desired location within the organism. Chemokine receptors are divided into different families, CXC chemokine receptors, CC chemokine receptors,CX3C chemokine receptors and XC chemokine receptors that correspond to the 4 distinct subfamilies of chemokines they bind. Specific chemokine receptors provide the portals for HIV to get into cells, and others contribute to inflammatory diseases and cancer.

CCR Inhibitors & Modulators (17)

Product Name Catalog No. Brief Description
BX471

HY-12080

BX471 is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1); exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

BX471 hydrochloride

HY-12080A

BX471 Hcl is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1); exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

Cenicriviroc

HY-14882

Cenicriviroc is an oral, dual CCR2/CCR5 antagonist, and displays potent anti-inflammatory and aninfective activity.

INCB 3284

HY-15450A

INCB 3284 is a potent, selective and orally bioavailable hCCR2 antagonist with IC50 of 3.7 nM(inhibition of monocyte chemoattractant protein-1 binding to hCCR2).

INCB 3284 dimesylate

HY-15450

INCB 3284 is a potent, selective and orally bioavailable hCCR2 antagonist with IC50 of 3.7 nM.

INCB3344

HY-50674

INCB3344 is a novel, potent and selective small molecule antagonist of the mouse CCR2 receptor; inhibits the binding of CCL2 to mouse monocytes with nanomolar potency (IC50 = 10 nM).

Maraviroc

HY-13004

Maraviroc (UK-427857; Selzentry; Celsentri) is a selective CCR5 antagonist (IC50= 6.4 nM); displays potent anti-HIV-1 activity.

MK-0812

HY-50669

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

MK-0812 Succinate

HY-50669A

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

NSC5844

HY-100033

NSC5844 (RE640) is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic properties.

PF-4136309

HY-13245

INCB8761(PF-4136309) is  a potent, Selective, and orally bioavailable CCR2 antagonist.

RS 504393

HY-15418

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively).

RS102895

HY-18611A

RS102895 is a potent and specific CCR2 antagonist with binding IC50 of 360 nM, no significant inhibition on CCR1(IC50 > 17 uM).

RS102895 hydrochloride

HY-18611

RS102895 Hcl is a potent and specific CCR2 antagonist with binding IC50 of 360 nM, no significant inhibition on CCR1(IC50 > 17 uM).

TAK-220

HY-19974

TAK-220 is an orally bioavailable small-molecule CCR5 antagonist.

Vercirnon

HY-15724

Vercirnon is a highly potent antagonist of CCR9, which has been implicated in the aetiology of inflammatory bowel diseases such as Crohn's disease.

Vicriviroc maleate

HY-17377

Vicriviroc maleate(Sch-417690) is a CCR5 antagonist with IC50 of 0.91 nM in clinical development for the treatment of HIV-1.