BCX 1470 methanesulfonate inhibits the esterolytic activity of factor D and C1s (IC50: 96 nM and 1.6 nM), 3.4- and 200-fold better than that of trypsin, respectively.
Factor D inhibitor 6 is a potent, highly selective, orally active compound that specifically inhibits the activity of factor D (FD). It demonstrates an IC50 of 30 nM and a Kd of 6 nM. Notably, Factor D inhibitor 6 does not exhibit any inhibitory effects against factor B, classical and lectin complement-pathway activation, nor does it interfere with a broad array of receptors, ion channels, kinases, and proteases.
Complement factor D-IN-1 is an effective and selective small-molecule reversible factor d inhibitor (IC50s: 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively).
c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, a kinase inhibitor of FMS (Colony-stimulating factor-1 receptor, CSF-1R; IC50: 2 nM) with anti-tumor activity.
FD-IN-1 is a factor D (FD) inhibitor with an IC50 of 12 nM.FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5μM, respectively. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system.
D-Mannuronic Acid is a blocker of the TLR2 and TLR4 downstream signaling pathway. D-Mannuronic Acid effectively inhibits mRNA expression of MyD88 and p65, major subunit of nuclear factor-kappaB.