Zilucoplan
- Product Name
- Zilucoplan
- CAS No.
- 1841136-73-9
- Chemical Name
- Zilucoplan
- Synonyms
- RA101495;Zilucoplan;Zilucoplan sodium;Poly(oxy-1,2-ethanediyl), α-[2-[[(4S)-4-carboxy-1-oxo-4-(1-oxohexadecyl)butyl]amino]ethyl]-ω-hydroxy-, 15-ether with N-acetyl-L-lysyl-L-valyl-L-α-glutamyl-L-arginyl-L-phenylalanyl-L-α-aspartyl-N-methyl-L-α-aspartyl-3-methyl-L-valyl-L-tyrosyl-3-(1H-pyrrolo[2,3-b]pyridin-3-yl)-L-alanyl-L-α-glutamyl-L-tyrosyl-L-prolyl-(2S)-2-cyclohexylglycyl-N6-(3-hydroxy-1-oxopropyl)-L-lysine (6→1)-lactam
- CBNumber
- CB99704201
- Molecular Formula
- (C2H4O)nC126H186N24O32
- Formula Weight
- 0
- MOL File
- 1841136-73-9.mol
Zilucoplan Property
- form
- Solid
- color
- White to off-white
Zilucoplan Chemical Properties,Usage,Production
Uses
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)[1][2].
in vivo
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].
| Animal Model: | C57BL/10SnJ C5-deficient (C5def) mice with anti-HMGCR+ IMNM IgG xenografts[1] |
| 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[1] |
| 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. |
References
[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. DOI:10.3390/biomedicines10082036
[2] Gorman DM, et, al. Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan. Amino Acids. 2021 Jan;53(1):143-147. DOI:10.1007/s00726-020-02921-5
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