Zilucoplan, TFA salt, INHIBITOR of Complement C5 inhibitor, CAS No.1841136-73-9 (free base), INHIBITOR of Complement C5 inhibitor

CAS: 1841136-73-9 (free base) Cat. No.: rp175435

GRADE & PURITY BioReagent, ≥98%(HPLC)

Overview

Zilucoplan TFA is a 15-amino acid synthetic macrocyclic peptide and a potent inhibitor of complement component 5 (C5), that blocks the cleavage of complement C5 into C5a and C5b which occurs as a consequence of activation of the classical, alternative, or lectin pathways. This mechanism of action inhibits formation of the membrane attack complex (MAC). Zilucoplan TFA can be used in research of immune-mediated necrotising myopathy (IMNM) . 

Formula: C₁₇₂H₂₇₈N₂₄O₅₅·xC₂HF₃O₂

Summary of Clinical Use

Zilucoplan was progressed to clinical evaluation in paroxysmal nocturnal hemoglobinuria (PNH) and generalized myasthenia gravis (gMG). Click here to link to ClinicalTrials.gov's full list of zilucoplan trials. The earliest approval for gMG was issued in Japan in September 2023, with FDA approval following in October, and EMA authorisation in December. In response to the SARS-CoV-2 pandemic plans were made to evaluate zilucoplan in COVID-19 patients, as part of the UK's Accelerating COVID-19 Research and Development (ACCORD) initiative (June 2020). ACCORD aims to fast-track potential treatments for COVID-19 through early-stage clinical trials. The first candidate agents included in the ACCORD study were 10478, MEDI3506 (tozorakimab, and anti-IL33 mAb), acalabrutinib, zilucoplan and nebulised heparin. Through this study researchers would aim to determine if the anti-inflammatory action mediated by zilucoplan has efficacy to reduce mortality in patients with severe COVID-19. In October 2023 the FDA approved zilucoplan to treat gMG in patients with acetylcholine receptor autoantibodies.  

Immunopharmacology Comments

Zilucoplan is a terminal complement inhibitor that has demonstrated promising clinical efficacy in patients with autoimmune myasthenia gravis. The functional effect of zilucoplan (i.e. inhibition of membrane attack complex formation) is comparable with the effect of the anti-C5 monoclonal eculizumab that is an approved PNH and generalized myasthenia gravis therapeutic.

Specifications

Product Name

Zilucoplan, TFA salt, INHIBITOR of Complement C5 inhibitor, CAS No.1841136-73-9 (free base)

Synonyms

YG391PK0CC | GTPL10404 | Zilucoplan [USAN] | DTXSID301336930 | Zilucoplan [USAN:INN] | 1841136-73-9 | WHO 10602 | Zilucoplan [INN] | UNII-YG391PK0CC | ZILUCOPLAN [WHO-DD] | Zilucoplan | RA101495 | RA101495 | RA3193 | DB15636

Grade

BioReagent

Specifications & Purity

BioReagent, ≥98%(HPLC)

Predicted molecular weight

3562.2 (free base)

Action Type

INHIBITOR

Mechanism of action

INHIBITOR of Complement C5 inhibitor

CAS

1841136-73-9 (free base)

Molecule Type

Peptide

Storage and Shipping

Storage

Protected from light,Store at -20°C,Desiccated,Avoid repeated freezing and thawing

Shipped In

Ice chest + Ice pads

Stability And Storage

Store at -20℃ long term (24 months). Avoid freeze/thaw cycle. Store in the dark. Desiccated.

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Organic acids and derivatives
    • Class Carboxylic acids and derivatives
      • Subclass Amino acids, peptides, and analogues
        • Level5 Peptides
          • Level6 Oligopeptides

• Kingdom: Organic compounds
• Superclass: Organic acids and derivatives
• Class: Carboxylic acids and derivatives
• Subclass: Amino acids, peptides, and analogues
• Intermediate Tree Nodes: Peptides
• Direct Parent: Oligopeptides
• Alternative Parents: Cyclic peptides Tyrosine and derivatives Phenylalanine and derivatives Pentacarboxylic acids and derivatives Glutamine and derivatives Glutamic acid and derivatives Aspartic acid and derivatives Valine and derivatives Proline and derivatives N-acyl-L-alpha-amino acids Macrolactams Alpha amino acid amides Amphetamines and derivatives Pyrrolopyridines Pyrrolidinecarboxamides N-acylpyrrolidines 1-hydroxy-2-unsubstituted benzenoids Substituted pyrroles Pyridines and derivatives N-acyl amines Tertiary carboxylic acid amides Heteroaromatic compounds Acetamides Secondary carboxylic acid amides Lactams Guanidines Dialkyl ethers Carboxylic acids Carboximidamides Azacyclic compounds Organopnictogen compounds Organic oxides Imines Hydrocarbon derivatives Carbonyl compounds
• Molecular Framework: Aromatic heteropolycyclic compounds
• Substituents: Alpha-oligopeptide - Cyclic alpha peptide - Tyrosine or derivatives - Phenylalanine or derivatives - Pentacarboxylic acid or derivatives - Glutamine or derivatives - Glutamic acid or derivatives - Aspartic acid or derivatives - Valine or derivatives - Proline or derivatives - N-acyl-l-alpha-amino acid - N-acyl-alpha amino acid or derivatives - N-acyl-alpha-amino acid - Macrolactam - Alpha-amino acid amide - Amphetamine or derivatives - Alpha-amino acid or derivatives - N-substituted-alpha-amino acid - Pyrrolopyridine - Pyrrolidine-2-carboxamide - Pyrrolidine carboxylic acid or derivatives - N-acylpyrrolidine - 1-hydroxy-2-unsubstituted benzenoid - Phenol - Fatty acyl - Benzenoid - Substituted pyrrole - Pyridine - N-acyl-amine - Fatty amide - Monocyclic benzene moiety - Heteroaromatic compound - Acetamide - Tertiary carboxylic acid amide - Pyrrolidine - Pyrrole - Secondary carboxylic acid amide - Lactam - Guanidine - Carboxamide group - Azacycle - Organoheterocyclic compound - Carboximidamide - Ether - Dialkyl ether - Carboxylic acid - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Imine - Carbonyl group - Aromatic heteropolycyclic compound
• Description: This compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
• External Descriptors: Not available

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

Genetic information

• Alternate Names: YG391PK0CC | GTPL10404 | Zilucoplan [USAN] | DTXSID301336930 | Zilucoplan [USAN:INN] | 1841136-73-9 | WHO 10602 | Zilucoplan [INN] | UNII-YG391PK0CC | ZILUCOPLAN [WHO-DD] | Zilucoplan | RA101495 | RA101495 | RA3193 | DB15636
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