chemokine receptor

Pirfenidone (AMR69) inhibits the production of CCL2 and CCL12 in fibroblasts and also decreases TGF-β2 protein levels. Pirfenidone is an antifibrotic agent that is commonly used in studies related to pulmonary fibrosis and also has anti-inflammatory activity.

C-021 dihydrochloride is a potent CCR4 antagonist that effectively inhibits functional chemotaxis in humans and mice, with IC50 values of 140 nM and 39 nM, respectively.

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

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.

β-NETA (α-NETA) is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM and is a potent chemokine-like receptor-1 (CMKLR1) antagonist. β-NETA has anti-cancer activity[1][2]. β-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM).

C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).

Cosalane (NSC 658586) is an HIV replication inhibitor, an inhibitor of chemokine receptor 7 (CCR7) signalling in humans and mice, with antiviral activity that blocks the binding of CCR7 to its natural ligands, CCL19 and CCL21.

AZD8309 is a potent, orally available antagonist of the chemokine receptor CXCR2 that regulates neutrophil transport, significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas.AZD8309 can be used to study a range of inflammatory diseases.

Ancriviroc (SCH-351125) is an oxime-piperidine compound with strong antiretroviral activity and an orally bioavailable small molecule chemokine receptor CCR5 antagonist (Kd value 9.27nM) that enters HIV-1 through the CCR5 co-receptor and is used to study HIV-1.

α-NETA is a potent choline acetyltransferase (ChA) inhibitor and an ALDH1A1 and chemokine-like receptor 1 (CMKLR1) antagonist.Anti-cancer activity,Cholinesterase and acetylcholinesterase (AChE) inhibition,Dose-dependent reduction of body weight and fasting blood glucose levels in STZ-induced diabetic mice,Significantly reduced expression of renal injury markers,May be CEP-9722 can be used for the study of diabetic nephropathy.

Delmetacin (Demethacin) is a non-steroidal anti-inflammatory compound with anti-inflammatory and analgesic activity and inhibitory effects on the CXC chemokine receptor CXCR1.

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

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

Bindarit is a selective inhibitor of monocyte chemoattractant proteins MCP-1 CCL2, MCP-3 CCL7 and MCP-2 CCL8 with anti-inflammatory effects. Bindarit specifically inhibits p65- and p65 p50-induced MCP-1 promoter activation and has no effect on other tested activated promoters.

Navarixin (MK-7123)(SCH527123) is a novel, selective CXC chemokine receptor 2(CXCR2) antagonist that inhibits neutrophil activation and modulates neutrophil trafficking in animal models, characteristics that may be beneficial in the treatment of conditions with unbalanced pulmonary neutrophilia.

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.

Vicriviroc maleate (SCH-417690 (maleate))(Sch-417690) is a piperazine-based CCR5 receptor antagonist with activity against human immunodeficiency virus. The IC50 value is 0.91 nM in clinical development for the treatment of HIV-1.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.

AZ084 is a potent, selective, allosteric, and orally active CCR8 antagonist (Ki: 0.9 nM) with potential to treat asthma.

CCR1 antagonist 7 (compound 16r) is a chemokine receptor 1 (CCR1) antagonist with an IC50 of 4 nM [1].

CCR4 antagonist 2 (Compound 31) is a novel, potent, orally bioavailable small molecule antagonist of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+ flux and [chemotaxis] CTX at 40 nM and 70 nM, respectively.

CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. This thiadiazole-dioxide ligand suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.

CRTh2 antagonist 3 is a powerful chemokine receptor homologous molecule expressed on Th2 cell (CRTh2) antagonists. CRTh2 antagonist 3 enhanced the activity of PDK1 on short peptide substrates with EC50 of 2 μM and Kd of 8.4 μM. CRTh2 antagonist 3 has the

CXCR7 modulator 2 is a 7-type C-X-C chemokine receptor (CXCR7) modulator with a Ki of 13 nM.