mip-1α-ccr5

TAK-220 is a selective and orally bioavailable CCR5 antagonist with IC50 values of 3.5 nM for RANTES binding inhibition and 1.4 nM for MIP-1α binding inhibition to CCR5.

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.

Fuscin is a quinonoid fungal metabolite originally isolated from O. fuscum that has diverse biological activities. It inhibits binding of the ADP/ATP translocase inhibitor atractyloside to rat liver mitochondria in an ADP-dependent manner when used at a concentration of 50 μM in a radioligand binding assay. Fuscin (20 μM) reduces the glutathione content of rat liver mitochondria to 28% of controls and inhibits NADH oxidation in sonicated pigeon heart mitochondria preparations in a concentration-dependent manner. It competes with macrophage inflammatory protein 1α (MIP-1α) for binding to CCR5 chemokine receptors in vitro with an IC50 value of 21 μM.

Maraviroc (UK-427857, Selzentry) belongs to small molecule drugs and is a C-C chemokine receptor 5 antagonist with oral activity and selectivity. This compound is used for the treatment of HIV-1 infection and has also shown anti-inflammatory, neuroprotective, and potential antitumor synergistic effects in research.

TAK-779 (Takeda 779) is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).