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| 5mg |
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| Targets |
ARC186 targets complement component C5. As an aptamer, it binds to C5 with high affinity and specificity, blocking its activation by the C5 convertase enzyme complex. This inhibition prevents the cleavage of C5 into C5a and C5b, thereby halting the downstream terminal complement cascade. By inhibiting C5 activation, ARC186 reduces the formation of the membrane attack complex (C5b‑9) and the anaphylatoxin C5a, which are key mediators of complement‑driven inflammation and cell lysis.
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| ln Vitro |
ARC186 is a potent complement inhibitor that blocks convertase‑catalyzed activation of C5. As a PEGylated nucleic acid aptamer with an identical sequence to avacincaptad pegol (ARC1905), it exhibits high‑affinity binding to C5. No specific IC₅0 values for C5 binding are reported. The 40 kDa PEG moiety improves the aptamer‘s pharmacokinetic properties, including extended circulation half‑life and reduced renal clearance, while the sodium salt form enhances solubility.
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| ln Vivo |
No specific in vivo activity data for ARC186 sodium are reported in the search results. However, its structural analog avacincaptad pegol (ARC1905) has been studied in clinical trials for geographic atrophy (GA) secondary to age‑related macular degeneration (AMD) and other complement‑mediated diseases. As a C5 inhibitor, ARC186 would be expected to reduce complement activity in vivo, with potential applications in ocular diseases, PNH, and other complement‑driven disorders.
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| Enzyme Assay |
The binding of ARC186 to complement C5 is measured by standard in vitro aptamer‑binding assays using purified recombinant human C5 protein. Surface plasmon resonance (SPR) or biolayer interferometry (BLI) can be used to determine binding affinity (KD). A competition assay using a labeled C5 ligand (e.g., fluorescently labeled C5) and unlabeled ARC186 is also used. The compound is characterized by HPLC and mass spectrometry to confirm purity (typically ≥95%), sequence, and PEG conjugation.
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| Cell Assay |
For cellular assays, human whole blood or complement‑active serum is used. ARC186 sodium is added at graded concentrations (0.1‑1000 nM) and complement activation is triggered by an activator (e.g., zymosan, LPS, or a specific antibody). Complement activity is measured by a hemolysis assay (e.g., CH50 or AH50) or by measuring the concentration of terminal complement complex (TCC, C5b‑9) by ELISA. Inhibition of C5a generation can be assessed by C5a ELISA. No specific cellular protocols are described.
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| Animal Protocol |
No animal experiments for ARC186 sodium are described in the search results. For in vivo evaluation of complement inhibition, 6‑8‑week‑old female C57BL/6 mice could be used in a model of complement‑mediated disease, such as LPS‑induced endotoxemia or a passive hemolysis model. ARC186 would be administered intravenously (IV) or subcutaneously (SC) at doses of 1‑30 mg/kg. Blood would be collected at various time points for measurement of complement activity (CH50) and C5a levels by ELISA. No such data are provided.
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| ADME/Pharmacokinetics |
ARC186 sodium is a PEGylated nucleic acid aptamer with a molecular weight of approximately 40 kDa for the PEG conjugate (free acid MW of the aptamer alone is approximately 35 kDa). For storage, the lyophilized powder should be kept at -20 degC for up to 3 years, sealed and protected from light. For in vitro use, stock solutions in sterile water or PBS (1‑10 mg/mL) can be prepared and stored at -80 degC for up to 6 months. Avoid repeated freeze‑thaw cycles. No detailed PK parameters are reported for ARC186 itself; avacincaptad pegol has a long half‑life of approximately 7‑14 days in humans after intravitreal injection.
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| Toxicity/Toxicokinetics |
No specific toxicity data for ARC186 sodium are reported. As a research‑grade aptamer, it is not intended for human or veterinary use. The structural analog avacincaptad pegol (ARC1905) has been evaluated in clinical trials and has shown an acceptable safety profile, with the most common adverse events being injection‑related (e.g., conjunctival hemorrhage, eye pain). No LD₅0 or formal toxicology studies are available.
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| References | |
| Additional Infomation |
ARC186 sodium is a research‑grade PEGylated nucleic acid aptamer that blocks C5 activation. Aptamers are single‑stranded oligonucleotides that fold into specific three‑dimensional structures and bind to target proteins with high affinity and specificity, similar to antibodies. ARC186 was developed as part of a program targeting complement‑mediated diseases. The sodium salt form is used to improve solubility and stability. The compound is for research use only and has not received regulatory approval.
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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 |
| 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.) |
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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