产品
编 号：F747503
分子式：C172H278N24O55
分子量：3562.18
分子式：C172H278N24O55
分子量：3562.18
产品类型
规格
价格
是否有货
1mg
询价
询价
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CAS No: 1841136-73-9
产品详情
生物活性：
Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM).
体内研究：
Zilucoplan (RA101495; 10 mg/kg; S.C.; daily, for 6 d) prevents the development of immune-mediated necrotising myopathy (IMNM) in C5-deficient mice supplemented with human complement.Zilucoplan (10 mg/kg; S.C.; daily, for 6 d) has protection on myopathy prevention in C57BL/6 mice.Animal Model:C57BL/10SnJ C5-deficient (C5def) mice with anti-HMGCR+ IMNM IgG xenografts
Dosage:10 mg/kg
Administration:Subcutaneous injection; daily, for 6 days
Result:Prevented muscle strength loss in C5def mice with less complement deposition on myofibres and consequently less necrosis/regeneration.
Animal Model:C57BL/6 mice with anti-HMGCR+ IMNM IgG xenografts
Dosage:10 mg/kg
Administration:Subcutaneous injection; daily, for 6 days
Result:Prevented muscle weakness and reduced regenerated myofibres.Decreased necrotic cells as well as regenerating cells expressing foetal myosin.
体外研究：
Zilucoplan (RA101495; 1-1000 nM; 30 min) inhibit Lipopolysaccharides-induced increase in C5a plasma levels in human whole blood with an IC50 value of 474.5 pM. Zilucoplan has a 65.7% reduction in C5a plasma levels observed at a concentration of 1 nM.Zilucoplan bins to complement component 5 (C5) and blocks the downstream assembly of the membrane attack complex (MAC; C5b-9) by inhibiting the cleavage of C5 by the C5 convertase into C5a and C5b andbinding to preformed C5b to sterically block interaction with C6, thereby inhibiting the formation of membrane pores and subsequent cell death.
Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM).
体内研究：
Zilucoplan (RA101495; 10 mg/kg; S.C.; daily, for 6 d) prevents the development of immune-mediated necrotising myopathy (IMNM) in C5-deficient mice supplemented with human complement.Zilucoplan (10 mg/kg; S.C.; daily, for 6 d) has protection on myopathy prevention in C57BL/6 mice.Animal Model:C57BL/10SnJ C5-deficient (C5def) mice with anti-HMGCR+ IMNM IgG xenografts
Dosage:10 mg/kg
Administration:Subcutaneous injection; daily, for 6 days
Result:Prevented muscle strength loss in C5def mice with less complement deposition on myofibres and consequently less necrosis/regeneration.
Animal Model:C57BL/6 mice with anti-HMGCR+ IMNM IgG xenografts
Dosage:10 mg/kg
Administration:Subcutaneous injection; daily, for 6 days
Result:Prevented muscle weakness and reduced regenerated myofibres.Decreased necrotic cells as well as regenerating cells expressing foetal myosin.
体外研究：
Zilucoplan (RA101495; 1-1000 nM; 30 min) inhibit Lipopolysaccharides-induced increase in C5a plasma levels in human whole blood with an IC50 value of 474.5 pM. Zilucoplan has a 65.7% reduction in C5a plasma levels observed at a concentration of 1 nM.Zilucoplan bins to complement component 5 (C5) and blocks the downstream assembly of the membrane attack complex (MAC; C5b-9) by inhibiting the cleavage of C5 by the C5 convertase into C5a and C5b andbinding to preformed C5b to sterically block interaction with C6, thereby inhibiting the formation of membrane pores and subsequent cell death.
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