1. Immunology/Inflammation
  2. Complement System
  3. Factor D inhibitor 6

Factor D inhibitor 6 

Cat. No.: HY-122700
Handling Instructions

Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.

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Factor D inhibitor 6 Chemical Structure

Factor D inhibitor 6 Chemical Structure

CAS No. : 1386455-51-1

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Description

Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases[1].

IC50 & Target

IC50: 30 nM (Factor D)[1]
Kd: 6 nM (Factor D)[1]

In Vitro

Factor D inhibitor 6 (compound 6) effectively blocks both alternative pathway (AP)-mediated hemolysis in 10% human serum (IC50 = 6 nM) and AP-induced membrane-attack complex (MAC) formation in lepirudinanticoagulated 50% human whole blood (IC50 = 0.14 μM)[1].
Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC50 = 0.86 μM)[1].
Factor D inhibitor 6 (compound 6) inhibits both hemolysis and component 3 (C3) deposition on the surface of red blood cells (RBCs) with an IC50 value of 70 nM, consistent with inhibition of the AP amplification loop[1].

In Vivo

Factor D inhibitor 6 (Compound 6; 1-10 mg/kg; Oral gavage; once; C57Bl/6 mice) treatment dosed-ependently inhibits complement activation, with full inhibition at 10 mg/kg. Factor D inhibitor 6 shows sustained inhibition of LPS-induced AP activation for at least 8 h post-dose with an EC50 of 0.034 μM[1].

Animal Model: C57Bl/6 mice induced by lipopolysaccharide (LPS)[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: Oral gavage; once
Result: Dosed-ependently inhibited complement activation, with full inhibition at 10 mg/kg.
Molecular Weight

484.91

Formula

C₂₃H₂₂ClFN₆O₃

CAS No.

1386455-51-1

SMILES

O=C([[email protected]]1N(C(CN2N=C(C(N)=O)C3=C2C=NC=C3)=O)[[email protected]]4([H])C[[email protected]]4([H])C1)N[[email protected]@H](C5=CC=CC(Cl)=C5F)C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Factor D inhibitor 6Factor D inhibitor6Factor D inhibitor-6Complement SystemFactor-Dalternativepathwayorallycomponent-3LPSparoxysmal nocturnalhemoglobinuriaInhibitorinhibitorinhibit

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Factor D inhibitor 6
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