Description
Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC 50 s of 0.006 and 0.05 µM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively.In VitroThe highly specific S1 serine protease factor D (FD) plays a central role in the amplification of the complement alternative pathway (AP) of the innate immune system. Complement factor D-IN-1 (compound 2) shows similar potency against human and monkey FD (IC 50 s in FD thioesterolytic assays of 0.005 µM and in 50% serum MAC deposition assays of 0.011 µM for both human and monkey). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoComplement factor D-IN-1 displays an excellent oral PK profile in Sprague–Dawley rats and, following an oral dose (10 mg/kg) in Brown Norway rats, demonstrates a good distribution and sustained exposure in ocular tissues including the neural retina and the posterior eye cup (PEC), which comprises the sclera, retinal pigmented epithelium, and choroid. Mean exposure levels in plasma, the PEC, and the retina at 6 h after dosing are 0.36, 0.43, and 0.09 µM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 0.006 µM (FD), 0.05 µM (MAC)