Zilucoplan
Based on 1 Customer Validation
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).
For research use only. We do not sell to patients.
- Purity: 99.71%
- CAS No.: 1841136-73-9
- Formula: C172H278N24O55
- Molecular Weight:3562.18
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Zilucoplan (10 mg/kg; S.C.; daily, for 6 d) has protection on myopathy prevention in C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/10SnJ C5-deficient (C5def) mice with anti-HMGCR+ IMNM IgG xenografts[1]
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Dosage:10 mg/kg
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Administration:Subcutaneous injection; daily, for 6 days
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Result:Prevented muscle strength loss in C5def mice with less complement deposition on myofibres and consequently less necrosis/regeneration.
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Animal Model:C57BL/6 mice with anti-HMGCR+ IMNM IgG xenografts[1]
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Dosage:10 mg/kg
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Administration:Subcutaneous injection; daily, for 6 days
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Result:Prevented muscle weakness and reduced regenerated myofibres.
Decreased necrotic cells as well as regenerating cells expressing foetal myosin.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1841136-73-9
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Appearance Solid
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Molecular Weight 3562.18
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Formula C172H278N24O55
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Color White to off-white
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Synonyms
RA101495; RA3193
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (28.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.2807 mL | 1.4036 mL | 2.8073 mL | 7.0182 mL |
| 5 mM | 0.0561 mL | 0.2807 mL | 0.5615 mL | 1.4036 mL | |
| 10 mM | 0.0281 mL | 0.1404 mL | 0.2807 mL | 0.7018 mL | |
| 15 mM | 0.0187 mL | 0.0936 mL | 0.1872 mL | 0.4679 mL | |
| 20 mM | 0.0140 mL | 0.0702 mL | 0.1404 mL | 0.3509 mL | |
| 25 mM | 0.0112 mL | 0.0561 mL | 0.1123 mL | 0.2807 mL |
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