产品
编 号：F685290
分子式：C23H22ClFN6O3
分子量：484.91
分子式：C23H22ClFN6O3
分子量：484.91
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
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10mg
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结构图
CAS No: 1386455-51-1
产品详情
生物活性：
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.
体内研究：
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.Animal Model:C57Bl/6 mice induced by lipopolysaccharide (LPS)
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.
体外研究：
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).Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC50 = 0.86 μM).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.
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.
体内研究：
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.Animal Model:C57Bl/6 mice induced by lipopolysaccharide (LPS)
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.
体外研究：
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).Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC50 = 0.86 μM).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.
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