FD-IN-1 (Compound 12) 是一种有效的，具有口服活性的补体因子 D (FD) 抑制剂，IC₅₀ 为 12 nM。补体因子 D 是一种高特异性的 S1 丝氨酸蛋白酶，在先天免疫系统的替代补体途径中起着重要作用。FD-IN-1 还抑制因子 XIa (FXIa) 和类胰蛋白酶 β2，IC₅₀ 分别为 7.7 和 6.5 μM。

FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC 50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC 50 s of 7.7 and 6.5 μM, respectively.

Solid

FD-IN-1 (Compound 12) exhibits functional inhibition of AP activation (IC50=0.26 μM) in vitro in a membrane attack complex (MAC) deposition assay using 50% human whole blood (WB). has not independently confirmed the accuracy of these methods. They are for reference only.

FD-IN-1 (Compound 12) demonstrates systemic suppression of AP activation in a lipopolysaccharide-induced alternative complement pathway (AP) activation model as well as local ocular suppression in intravitreal injection-induced AP activation model in mice expressing human FD.
FD-IN-1 (Compound 12) exhibits high oral bioavailability (C57BL6 mice 83%, Beagle dogs 70%) following oral administration (mice and dogs 10 mg/kg).
FD-IN-1 (Compound 12) exhibits terminal elimination half-lives (C57BL6 mice 1.6 h and Beagle dogs 3.8 h) following intravenous administration (mice and dogs 1 mg/kg). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Karki RG, et al. Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway. J Med Chem. 2019 May 9;62(9):4656-4668.

In Vitro: DMSO : 62.5 mg/mL (165.59 mM; ultrasonic and warming and heat to 80°C)配制储备液