Pirfenidone D5 (AMR69 D5) is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
BMS-753426 is a potent and orally bioavailable antagonist of CCR2.
Maceneolignan H (Compound 8) is a neolignane compound isolated from the arils of Myristica fragrans. Maceneolignan H is a selective CCR3 antagonist (EC50 = 1.4 μM). Maceneolignan H has the potential for the research of allergic diseases[1].
AZD-4818 is a potent antagonist of chemokine CCR1. AZD-4818 can be used for the treatment of chronic obstructive pulmonary disease (COPD) [1].
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.
PF-07054894 is a potent CCR6 antagonist. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease[1].
FLX475 is a potent CCR4 antagonist that blocks regulatory T cells that interfere with effective antitumor immune responses and has antitumor activity[1].
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis[1][2][3].
CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease[1].
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 [1][2][3].
Ophiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells[1]. Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells[2].
MLN 3897 is a potent, specific and orally active antagonist of CCR1 with IC50 of 0.8 nM in competition binding assays, 500-fold selectivity over CCR5; inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-fos signaling, inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-Fos signaling; demonstrates potential for the treatment of multiple sclerosis and rheumatoid arthritis. Multiple Sclerosis Phase 1 Discontinued
Cosalane (NSC 658586) is a potent inhibitor of HIV replication. Cosalane has an intrinsic ability to block human and murine CCR7 function in vitro in response to both of its natural ligands, CCL19 and CCL21, with the IC50 of 0.207/2.66 μM in human for CCL19/CCL21 and 0.193/1.98 μM in murine, respectively[1][2].
Met-RANTES (human) is a partial antagonist of CCR5. Met-RANTES (human) reduces the infiltration of blood monocytes into the liver[1].
AZD 1678 is a potent, selective orally bioavailable CCR4 receptor antagonist with pIC50 of 8.6 for hCCR4, pIC50 of 9.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.8. Asthma Phase 1 Clinical
CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM.
Fuscin, a fungal metabolite, CCR5 receptor antagonist with anti-HIV effects. Fuscin is a respiration and oxidative phosphorylation inhibitor, and also a mitochondrial SH-dependent transport-linked functions inhibitor[1][2][3].
CCR8 antagonist 2 is a potent antagonist of CCR8. CCR8 (C-C Motif Chemokine Receptor 8) is predominantly expressed on Treg cells and Th2 cells, but not on Th1 cells. CCR8 antagonist 2 inhibits CCR8 activity, which may be used in the treatment of diseases mediated by CCR8, such as cancer, and/or neuropathic pain (extracted from patent WO2022000443A1, compound 220)[1].
(1S)-CCR2 antagonist 1 is a left-handed chiral body of CCR2 antagonist 1 (HY-112792). CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM[1].
IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research[1].
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.
(Rac)-PF-4136309 is an isoform of PF-4136309 (HY-13245), which 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.
Carlumab (CNTO 888) is a humanised anti-CCL2 (chemokine ligand 2) antibody with high affinity. Carlumab can be used in cancer research, particularly in prostate cancer[1].
C-021 dihydrochloride is a potent and orally bioavailable CCR4 antagonist with IC50 of 0.14 uM and 0.039 uM for inhibition of chemotaxis in human and mouse, respectively.
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). CKLF1-C19 interacts with CCR4, and inhibits chemotaxis induced by both CKLF1 and CCL17. CKLF1-C19 can suppress allergic lung inflammation via inhibiting chemotaxis mediated by CCR3 and CCR4[1].
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively[1].
Aplaviroc, a SDP derivative, is a CCR5 antagonist, with IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.
CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM.
RPT193 is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. RPT193 can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research[1].
CMPD167 (MRK-1) is an orally acitve small molecule that binds to CCR5 to inhibit gp120 association, inhibits different stages of the virus-cell attachment and entry process (CCR5-using virus SHIV-162P3, IC50<1 nM).