Zilucoplan TFA  (Synonyms: RA101495 TFA; RA3193 TFA)

Zilucoplan TFA (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan TFA can be used in research of immune-mediated necrotising myopathy (IMNM)^[1][2].

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^[2].
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 and binding to preformed C5b to sterically block interaction with C6, thereby inhibiting the formation of membrane pores and subsequent cell death^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].
Zilucoplan (10 mg/kg; S.C.; daily, for 6 d) has protection on myopathy prevention in C57BL/6 mice^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

3562.18 (free base)

C₁₇₂H₂₇₈N₂₄O₅₅.xC₂HF₃O₂

Room temperature in continental US; may vary elsewhere.

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

• [1]. Julien S, et, al. Prevention of Anti-HMGCR Immune-Mediated Necrotising Myopathy by C5 Complement Inhibition in a Humanised Mouse Model. Biomedicines. 2022 Aug 20;10(8):2036.  [Content Brief]

  [2]. Gorman DM, et, al. Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan. Amino Acids. 2021 Jan;53(1):143-147.  [Content Brief]