CCR Antagonist

BI 6901 is a potent, selective CCR10 antagonist (pIC₅₀=9.0). BI 6901 shows high selectivity over other GPCRs, including a number of other chemokine receptors. BI 6901 is efficacious in the murine DNFB model of contact hypersensitivity and can be used for inflammation research.

Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer.

CMKLR1 antagonist 1 (compound S-26d) is a potent and orally active chemokine-like receptor 1 (CMKLR1) antagonist, with a pIC₅₀ value of 7.44 in hCMKLR1-transfected CHO cells. CMKLR1 antagonist 1 can be used for psoriasis and metabolic diseases research.

AZD-1678 is a potent CCR4 receptor antagonist, with a pIC₅₀ of 8.6.

MLN3126 is an orally active and potent CCR9 antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis of mouse primary thymocytes, wiht an IC₅₀ value of 6.3 nM for calcium influx.

(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 K_i of 2.4 nM.

SCH 350581 (AD-101) is a CCR5 antagonist. SCH 350581 inhibits HIV-1 replication, viral entry into cells, and the binding of gp120 to cell lines in primary lymphocytes.

BMS-681 is an orthosteric antagonist of CC chemokine receptor 2 (CCR2). BMS-681 restricts the movement of the extracellular end of TM6 by stabilizing TM7. TM7 and TM6 are the main components of the orthosteric binding site. BMS-681 can be used to study inflammatory neurodegenerative diseases and cancer.

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits T_reg 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 are 40 nM and 70 nM, respectively.

CCR1 antagonist 6 (compound 16q) is a chemokine receptor 1 (CCR1) antagonist, with an IC₅₀ of 3 nM.

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

BMS-753426 is a potent and orally bioavailable antagonist of CCR2.

CCR1 antagonist 11 hydrochloride (A1B1) is an orally active CCR1 antagonist with the IC₅₀ values of 0.03 μM, 0.58 μM and 0.32 μM for hCCR1, mCCR1 and rCCR1, respectively. CCR1 antagonist 11 hydrochloride can be used in the study of rheumatoid arthritis and other related inflammatory diseases.

CCR5 antagonist 4 is an orally active CCR5 antagonist. CCR5 antagonist 4 can be studied in research on rheumatoid arthritis.

Maraviroc (Standard) is the analytical standard of Maraviroc. This product is intended for research and analytical applications. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.

Vicriviroc (SCH 417690) is an orally active CCR5 antagonist with the IC₅₀ of 10 nM, and also inhibts MIP-1α and intracellular calcium release induced by the ligand RANTES (10 nM) with the IC₅₀ values of 0.91 nM and 16 nM,,respectively. Vicriviroc can inhibits human immunodeficiency virus type 1 (HIV-1) infection, and can also used for study of cancer.

CXCR2/CCR7 antagonist-1 (compound 6) is a potent CXCR2 and CCR7 dual antagonist with IC₅₀s of 0.0046 and 0.0014 μM, respectively. CXCR2/CCR7 antagonist-1 can be used in the study of cancer metastasis and autoimmune diseases.

PF-232798 is an orally active CCR5 antagonist with anti-HIV effects.

(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.

Vicriviroc (SCH 417690) malate is an orally active CCR5 antagonist with the IC₅₀ of 10 nM, and also inhibts MIP-1α and intracellular calcium release induced by the ligand RANTES (10 nM) with the IC₅₀ values of 0.91 nM and 16 nM,,respectively. Vicriviroc malate can inhibits human immunodeficiency virus type 1 (HIV-1) infection, and can also used for study of cancer.