CCR

Mogamulizumab is a monoclonal antibody targeting CC chemokine receptor 4 with anticancer effects, used in ATLL and CTCL studies.

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM).

AZ084 is a potent, selective, allosteric, and oral active CCR8 antagonist (Ki: 0.9 nM). It has the potential to treat asthma.

CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

ML604086 suppresses CCL1 mediated chemotaxis and enhances intracellular Ca2 concentrations.

Leronlimab (PRO 140), a humanized IgG4 monoclonal antibody, targets CCR5 to combat HIV and cancer.

INCB-9471 is a CCR5 antagonist with anti-HIV activity and inhibits the interaction between HIV-1 gp120.

MK-0812 Succinate is an effective and selective CCR2 antagonist.

CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2.

Bertilimumab (CAT 213; iCo-008), humanized anti-eotaxin-1 mAb, inhibits eosinophil chemotaxis/activation for allergic disease research.

VZMC013 is a potent chemical probe targeting the MOR-CCR5 heterodimer, effectively inhibiting HIV-1 entry exacerbated by opioid compounds. It exhibits nanomolar binding affinity to both MOR and CCR5, inhibits CCL5-activated calcium mobilization, and significantly enhances anti-HIV-1BaL activity compared to previously reported bivalent ligands. In TZM-bl cells co-expressing CCR5 and MOR, VZMC013 demonstrates greater inhibition of viral infection than in cells expressing only CCR5. Additionally, VZMC013 blocks HIV-1 entry into peripheral blood mononuclear cells (PBMC) in a concentration-dependent manner and more effectively inhibits opioid-accelerated HIV-1 entry in phytohemagglutinin-activated PBMC than in opioid-free environments.

Met-RANTES (human) acetate is the acetate salt form of Met-RANTES (human). It acts as an antagonist for CCR1 and CCR5 receptors. This compound inhibits the human chemokines MIP-1α and MIP-1β, with respective IC₅₀ values of 5 and 2 nM. Additionally, Met-RANTES (human) acetate reduces bone destruction and alleviates adjuvant-induced arthritis (AIA) in rats.

INCB3344 is a potent CCR2 antagonist. INCB3344 R-isomer is the R-isomer of INCB3344.

MLN-3897 TFA is a potent CCR1 antagonist that inhibits the binding of 125I-MIP-1α to THP-1 cell membranes.

Orally active CCR4 antagonist with piperidinyl-azetidine; IC50: 22 nM (calcium flux), 50 nM (CTX); antitumor effects.

INCB 3284 dimesylate: oral CCR2 antagonist, blocks MCP-1/hCCR2 binding (IC50: 3.7 nM), potential in acute liver failure research.

Mip-IN-2 is a high-affinity MIP protein inhibitor that inhibits PPIase activity and reduces bacterial virulence for use in anti-infection research.

GSK163929 (compound 122) is an orally active CCR5 antagonist with anti-HIV properties and demonstrates low inhibitory potency against hEGR. Administered at a dosage of 2000 mg/kg/day (i.v., 7 d), it shows no adverse effects in rats, and at 250 mg/kg/day (i.v., 7 d), it is similarly non-toxic in dogs.

Aplaviroc, a potent CCR5 inhibitor, binds selectively, blocking HIV entry and specific monoclonal antibody attachment in vitro.