Complement factor D-IN-1 |
Catalog No.GC31846 |
보체 인자 D-IN-1은 FD Thioesterolytic Fluorescent Assay 및 MAC Deposition Assay에서 각각 IC50이 0.006 및 0.05μM인 강력하고 선택적인 소분자 가역성 인자 d 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1386455-76-0
Sample solution is provided at 25 µL, 10mM.
Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC50s of 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively.
The 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 (IC50s in FD thioesterolytic assays of 0.005 μM and in 50% serum MAC deposition assays of 0.011 μM for both human and monkey)[1].
Complement 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[1].
[1]. Lorthiois E, et al. Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D InhibitorsDemonstrating Alternative Complement Pathway Inhibition in Vivo. J Med Chem. 2017 Jul 13;60(13):5717-5735.
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