keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zilucoplan TFA (RA101495), a 15-amino acid macrocyclic peptide, serves as a potent inhibitor of complement component 5 (C5). It has applications in the study of immune-mediated necrotising myopathy (IMNM) [1] [2].
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Description | Zilucoplan TFA (RA101495), a 15-amino acid macrocyclic peptide, serves as a potent inhibitor of complement component 5 (C5). It has applications in the study of immune-mediated necrotising myopathy (IMNM) [1] [2]. |
In vitro | Zilucoplan (RA101495; 1-1000 nM; 30 min) suppresses the lipopolysaccharide-induced increase in C5a plasma levels in human whole blood, with an inhibitory concentration (IC50) of 474.5 pM. A 65.7% reduction in C5a plasma levels is achieved with a 1 nM concentration of Zilucoplan [2]. This compound binds to the complement component 5 (C5) and prevents the formation of the membrane attack complex (MAC; C5b-9) by inhibiting the cleavage of C5 into C5a and C5b and by binding to C5b, thereby hindering its interaction with C6. This action obstructs the assembly of MAC and the subsequent cell lysis [1]. |
In vivo | Zilucoplan (RA101495; 10 mg/kg; S.C.; daily for 6 days) effectively inhibits the onset of immune-mediated necrotising myopathy (IMNM) in C5-deficient mice treated with human complement and also offers protective benefits against myopathy in C57BL/6 mice [1]. |
Synonyms | RA101495 TFA |
Molecular Weight | 3562.18 (free base) |
Formula | (C2H4O)nC126H186N24O32.C2HF3O2 |
keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Zilucoplan TFA Immunology/Inflammation Complement System RA101495 TFA inhibitor inhibit