产品
编 号：F198307
分子式：C23H23NO4
分子量：377.43
分子式：C23H23NO4
分子量：377.43
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 1646682-14-5
产品详情
生物活性：
FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 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 IC50s of 7.7 and 6.5 μM, respectively.
体内研究：
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).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.
体外研究：
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).
FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 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 IC50s of 7.7 and 6.5 μM, respectively.
体内研究：
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).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.
体外研究：
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).
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