| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Complement component C5. ARC186 blocks the convertase-catalyzed activation of C5, thereby preventing the formation of the membrane attack complex (MAC) and downstream complement activation. This mechanism inhibits both the classical and alternative complement pathways.
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| ln Vitro |
No detailed in vitro data available. As an aptamer-based C5 inhibitor, ARC186 is expected to bind to human C5 with high affinity and specificity, preventing its cleavage into C5a and C5b. This activity can be measured in serum-based complement activity assays such as CH50 or AP50.
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| ln Vivo |
In preclinical models, ARC186 has shown efficacy in complement-mediated diseases. Antisense oligonucleotides targeting factor B (a related complement protein) have demonstrated reductions in plasma factor B levels and improved renal pathology in lupus nephritis models.
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| Enzyme Assay |
Surface plasmon resonance (SPR) or biolayer interferometry (BLI) using immobilized C5 protein is used to measure binding affinity. Alternatively, complement functional assays: human serum is incubated with ARC186, then complement activation is triggered (e.g., by zymosan or aggregated IgG). C5a or sC5b-9 levels in supernatant are measured by ELISA.
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| Cell Assay |
Cells expressing C5 or complement receptors are not typical. For cellular assays, human whole blood or serum is incubated with ARC186, and complement-dependent cell lysis (e.g., of sensitized sheep red blood cells in hemolytic assays) is measured spectrophotometrically. Not a cell-based assay in the traditional sense.
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| Animal Protocol |
In rodent models of complement-mediated disease (e.g., lupus nephritis, paroxysmal nocturnal hemoglobinuria), ARC186 is administered via intravenous injection. Dosing regimens vary by study. Endpoints include complement activity in serum (CH50), proteinuria, renal histopathology, and survival.
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| ADME/Pharmacokinetics |
As a PEGylated oligonucleotide aptamer, ARC186 has a prolonged plasma half-life due to PEG conjugation, which reduces renal clearance and protects against nuclease degradation. Pharmacokinetic studies are expected to show stability in circulation with distribution primarily in plasma and extracellular fluid.
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| Toxicity/Toxicokinetics |
No detailed toxicity data reported in the literature. Aptamer-based therapies generally have favorable safety profiles with minimal immunogenicity. PEGylated aptamers may show reduced off-target effects compared to small molecules. Standard handling precautions for oligonucleotides apply.
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| References | |
| Additional Infomation |
ARC186 is a research-grade aptamer, not FDA-approved for clinical use. It is identical in sequence to avacincaptad pegol (ARC1905), which has been investigated in clinical trials for geographic atrophy. ARC186 is strictly for research use and is not intended for human therapeutic applications.
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| Molecular Weight |
12702.76
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|---|---|
| Appearance |
White to off-white solid powder
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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) |
H2O :~100 mg/mL (~7.87 mM)
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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 | 0.0787 mL | 0.3936 mL | 0.7872 mL | |
| 5 mM | 0.0157 mL | 0.0787 mL | 0.1574 mL | |
| 10 mM | 0.0079 mL | 0.0394 mL | 0.0787 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.
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