CCR1 Antagonist

BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a K_i of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

RS102895 is a potent CCR2 antagonist, with an IC₅₀ of 360 nM, and shows no effect on CCR1.

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with K_i of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

RS102895 hydrochloride is a potent CCR2 antagonist, with an IC₅₀ of 360 nM, and shows no effect on CCR1.

J-113863 is a potent and selective CCR1 antagonist with IC₅₀ values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. 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). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.

MLN3897 is an orally active CCR1 antagonist. MLN3897 inhibits the c-fos and Akt pathways by blocking the binding of CCL3 to CCR1, thereby reducing immune cell infiltration, attenuating osteoclasts, and interfering with tumor-microenvironment interactions. MLN3897 can be used in research on multiple myeloma, multiple myeloma bone disease, and rheumatoid arthritis.

BX-513 (VUF2274) is a CCR1 antagonist that inhibits chemokine binding and blocks US28 signaling. BX-513 inhibits human CCR1 with a K_i of 40 nM. BX-513 blocks CCL3-mediated signaling/chemotaxis, CCR1-mediated chemokine signaling, calcium mobilization, extracellular acidification, and US28-mediated HIV entry, with an IC₅₀ of 4.9 μM. BX-513 can be used for research on hcmv infection.

YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the K_i values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.

Met-RANTES (human) acetate is the acetate form of Met-RANTES (human) (HY-P4191). Met-RANTES (human) acetate is the antagonist for CCR1 and CCR5. Met-RANTES (human) acetate inhibits chemokines human MIP-1α and MIP-1β with IC₅₀ of 5 and 2 nM. Met-RANTES (human) acetate reduces bone destruction and ameliorates rats adjuvant-induced arthritis (AIA).

CCX354 is an antagonist of CCR1, with anti-inflammatory activity.

BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC₅₀), respectively. BMS-817399 can be used for the research of rheumatoid arthritis.

BI 639667 (compound 19n), a chemical probe, is a CCR1 antagonist, with an IC₅₀ of 1.8 nM in Ca²⁺ flux assay.

CCR1 antagonist 9 is a potent and selective CCR1 antagonist with an IC₅₀ of 6.8 nM in calcium flux assay.

BX-513 hydrochloride (VUF2274 hydrochloride) is a CCR1 antagonist that inhibits chemokine binding and blocks US28 signaling. BX-513 hydrochloride inhibits human CCR1 with a K_i of 40 nM. BX-513 hydrochloride blocks CCL3-mediated signaling/chemotaxis, CCR1-mediated chemokine signaling, calcium mobilization, extracellular acidification, and US28-mediated HIV entry, with an IC₅₀ of 4.9 μM. BX-513 hydrochloride can be used for research on hcmv infection.

Met-RANTES (human) is the antagonist for CCR1 and CCR5. Met-RANTES (human) inhibits chemokines human MIP-1α and MIP-1β with IC₅₀ of 5 and 2 nM. Met-RANTES (human) reduces bone destruction and ameliorates rats adjuvant-induced arthritis (AIA).

CP-481715 is a potent, reversible and selective CCR1 antagonist with a K_d of 9.2 nM for human CCR1. CP-481715 is >100-fold selective for CCR1 as compared with a panel of G-protein-coupled receptors including related chemokine receptors. CP-481715 has the potential for rheumatoid arthritis and other inflammatory diseases research.

CCR1 antagonist 12 (Compound 12) is an antagonist for CCR1 with IC₅₀ of 3 nM for human CCR1. CCR1 antagonist 12 inhibits CCL3-induced transwell chemotaxis with an IC₅₀ of 0.009 µM. CCR1 antagonist 12 exhibits good pharmacokinetic characters in rats model.

CCR1 antagonist 13 is a selective CCR1 small molecule antagonist.

CCR1 antagonist 10 (example 1) is a potent and orally active CCR1 antagonist. CCR1 antagonist 10 inhibits ¹²⁵I-MIP-1α binding to THP-1 cell membranes with an K_i value of 2.3 nM.

CP-865569 is a CCR1 antagonist. CP-865569 can be used in the research of inflammatory diseases and autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis.