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Complement?factor?D-IN-1

CAS No. : 1386455-76-0

MCE 站：Complement?factor?D-IN-1

产品活性：Complement factor D-IN-1是一种有效的和选择性的小分子可逆因子(small-molecule reversible factor d) 抑制剂，在FD硫酯分解荧光实验和MAC沉积测定中IC₅₀值分别为0.006 和 0.05 μM。

研究领域：Others

作用靶点：Others

In Vitro: 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).

In Vivo: 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.

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