| Identification | Back Directory | [Name]
FD-IN-1 | [CAS]
1646682-14-5 | [Synonyms]
FD-IN-1
Benzeneacetic acid, 2-[[3'-[(1S)-1-amino-2-hydroxyethyl][1,1'-biphenyl]-3-yl]methoxy]-
(S)-2-(2-((3'-(1-amino-2-hydroxyethyl)-[1,1'-biphenyl]-3-yl)methoxy)phenyl)acetic acid | [Molecular Formula]
C23H23NO4 | [MDL Number]
MFCD32067952 | [MOL File]
1646682-14-5.mol | [Molecular Weight]
377.43 |
| Chemical Properties | Back Directory | [Boiling point ]
629.4±55.0 °C(Predicted) | [density ]
1.251±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
4.14±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
FD-IN-1 (Compound 12) is a potent, orally active complement factor D (FD) inhibitor with IC50 of 12 nM.It also inhibits factor XIa (FXIa) and tryptase β2 with IC50 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). | [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). b> | 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. | table>
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MedChemExpress
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www.medchemexpress.com |
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Tags:1646682-14-5
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