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1mg |
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Other Sizes |
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ln Vitro |
With an IC50 value of 474.5 pM, zilucoplan (RA101495; 1-1000 nM; 30 min) inhibits the increase in C5a plasma levels in human whole blood caused by lipopolysaccharides. When zilucoplan is used at a concentration of 1 nM, C5a plasma levels are reduced by 65.7% [2]. By preventing C5 from being broken down by C5 convertase into C5a and C5b and attaching to preformed C5b to sterically block interaction with C6, zilucoplan binds to complement component 5 (C5) and prevents the downstream assembly of the membrane attack complex (MAC; C5b-9)[1].
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ln Vivo |
In C5-deficient mice treated with human complement, zilucoplan (RA101495; 10 mg/kg; SC; daily, for 6 d) inhibits the development of immune-mediated necrotizing myopathy (IMNM)[1]. In C57BL/6 mice, zilucoplan (10 mg/kg; SC; daily, for 6 d) shows protective effects on the prevention of myopathy[1].
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Animal Protocol |
Animal/Disease Models: C57BL/10SnJ C5-deficient (C5def) mice with anti-HMGCR+ IMNM IgG xenografts[1]
Doses: 10 mg/kg Route of Administration: subcutaneous (sc) injection; daily, for 6 days Experimental Results: Prevented muscle strength loss in C5def mice with less complement deposition on myofibres and consequently less necrosis/regeneration. Animal/Disease Models: C57BL/6 mice with anti-HMGCR+ IMNM IgG xenografts[1] Doses: 10 mg/kg Route of Administration: subcutaneous (sc) injection; daily, for 6 days Experimental Results: Prevented muscle weakness and decreased regenerated myofibres. diminished 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.
[2]. Gorman DM, et, al. Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan. Amino Acids. 2021 Jan;53(1):143-147. |
Molecular Formula |
C172H278N24O55
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Molecular Weight |
3562.18
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CAS # |
1841136-73-9
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Related CAS # |
Zilucoplan TFA
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C([C@H](C1CCCCC1)NC([C@@H]1CCCN1C([C@H](CC1C=CC(=CC=1)O)NC([C@H](CCC(=O)O)NC([C@H](CC1=CNC2C1=CC=CN=2)NC([C@H](CC1C=CC(=CC=1)O)NC([C@H](C(C)(C)C)NC([C@H](CC(=O)O)N(C)C([C@@H]1CC(NCCCC[C@@H](C(N[C@H](C(N[C@@H](CCC(=O)O)C(N[C@@H](CCCNC(=N)N)C(N[C@@H](CC2C=CC=CC=2)C(N1)=O)=O)=O)=O)C(C)C)=O)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)N[C@H](C(=O)O)CCCCNC(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(CC[C@@H](C(=O)O)NC(CCCCCCCCCCCCCCC)=O)=O)=O
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Synonyms |
Zilbrysq
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.2807 mL | 1.4036 mL | 2.8073 mL | |
5 mM | 0.0561 mL | 0.2807 mL | 0.5615 mL | |
10 mM | 0.0281 mL | 0.1404 mL | 0.2807 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.