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。

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.

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IC50: 0.006 μM (FD), 0.05 μM (MAC)

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). has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 250 mg/mL (517.26 mM; Need ultrasonic)配制储备液