计算溶液所需的质量、体积或浓度。
概述
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.
In Vitro
FD-IN-1 (Compound 12) exhibits functional inhibition of AP activation (IC 50 =0.26 μM) in vitro in a membrane attack complex (MAC) deposition assay using 50% human whole blood (WB). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Human FD knock-in mice Dosage: 3 and 10 mg/kg Administration: Oral gavage Result: The AP pathway was fully inhibited for up to 10 h at the 10 mg/kg dose.
规格
规格或纯度
10mM in DMSO
英文名称
FD-IN-1
生化机理
FD-IN-1 （化合物 12）是一种可口服的选择性因子 D（FD）抑制剂，其 IC 50 为 12 nM。补体 FD 是一种高度特异的 S1 丝氨酸蛋白酶，在先天性免疫系统的替代性补体途径中发挥着核心作用。FD
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
分子量
377.43
高级数据
质检证书(CoA,COO,BSE/TSE 和分析图谱)
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溶液计算器
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