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Zilucoplan

Cat. No. M11438
Zilucoplan Structure
Synonym:

RA101495

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1mg USD 545  USD545 In stock
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Quality Control & Documentation
Biological Activity

Zilucoplan is a 15 amino acid macrocyclic peptide and potent complement component 5 (C5) inhibitor that specifically targets C5, a component of the terminal complement activation pathway, thereby preventing the cleavage of C5 by C5 converting enzyme into complement components C5a and C5b, and thus preventing the downstream assembly and activity of the membrane attack complex (MAC). Can be used in studies related to immune-mediated necrotizing myopathy (IMNM) and generalized myasthenia gravis (gMG).

Chemical Information
Molecular Weight 3562
Formula C172H278N24O55
CAS Number 1841136-73-9
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] James F Howard Jr, et al. Expert Opin Investig Drugs. Zilucoplan: An Investigational Complement C5 Inhibitor for the Treatment of Acetylcholine Receptor Autoantibody-Positive Generalized Myasthenia Gravis

[2] Declan M Gorman, et al. Amino Acids. Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan

[3] Jozefien Declercq, et al. Trials. Zilucoplan in patients with acute hypoxic respiratory failure due to COVID-19 (ZILU-COV): A structured summary of a study protocol for a randomised controlled trial

[4] Marinos C Dalakas. Curr Opin Neurol. Progress in the therapy of myasthenia gravis: getting closer to effective targeted immunotherapies

[5] James F Howard Jr, et al. JAMA Neurol. Clinical Effects of the Self-administered Subcutaneous Complement Inhibitor Zilucoplan in Patients With Moderate to Severe Generalized Myasthenia Gravis: Results of a Phase 2 Randomized, Double-Blind, Placebo-Controlled, Multicenter Clinical Trial

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Keywords: Zilucoplan, RA101495 supplier, Complement System, inhibitors, activators


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