FD-IN-1_product_DataBase

Bioactivity

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[1].

Invitro

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)[1].

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[1].FD-IN-1 (Compound 12) exhibits high oral bioavailability (C57BL6 mice 83%, Beagle dogs 70%) following oral administration (mice and dogs 10 mg/kg)[1]. 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)[1]. Animal Model:

Name

FD-IN-1

CAS

1646682-14-5

Formula

C23H23NO4

Molar Mass

377.43

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

FD-IN-1

CAS: 1646682-14-5 F: C23H23NO4 W: 377.43