| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
In vitro, compstatin has a half-life of roughly two hours in human blood[2]. Compstatin creates a hydrophobic cluster in solution by producing a β-turn at residues Gln-5–Gly-8, Ile–1–Val–4, and Thr–13, along with the disulfide bridge Cys-2–Cys12[3].
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| ln Vivo |
When administered as a bolus injection plus infusion, compstatin (21 mg/kg) results in total suppression. Compstatin completely prevents complement activation generated by heparin and prostamine in vivo, however without changing heart rate or pulmonary, central venous, or systemic artery pressures [1]. In baboon plasma, compstatin is stable for more than 24 hours[1]. The group that received Compstatin perfusion had a considerably longer survival rate for pig xenografts than the control group [2].
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| Animal Protocol |
Animal/Disease Models: Juvenile baboons (P. Anubis) weighing 10.5-28.8 kg[1].
Doses: 50, 25 mg/kg 60 min after heparin and 2 min before protamine. Route of Administration: A bolus injection. Experimental Results: Completely inhibited complement activation induced by heparin–protamine complexes. |
| References |
[1]. Soulika AM, et al. Inhibition of heparin/protamine complex-induced complement activation by Compstatin in baboons. Clin Immunol. 2000 Sep;96(3):212-21.
[2]. Fiane AE, et al. Compstatin, a peptide inhibitor of C3, prolongs survival of ex vivo perfused pig xenografts. Xenotransplantation. 1999 Feb;6(1):52-65. [3]. Bert J C Janssen, et al. Structure of compstatin in complex with complement component C3c reveals a new mechanism of complement inhibition. J Biol Chem. 2007 Oct 5;282(40):29241-7. [4]. A Sahu, et al. Inhibition of human complement by a C3-binding peptide isolated from a phage-displayed random peptide library. J Immunol. 1996 Jul 15;157(2):884-91. |
| Molecular Formula |
C68H100F3N23O19S2
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|---|---|
| Molecular Weight |
1664.79
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| Related CAS # |
Compstatin;206645-99-0
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~60.07 mM)
H2O :~50 mg/mL (~30.03 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (1.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (1.65 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (1.65 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6007 mL | 3.0034 mL | 6.0068 mL | |
| 5 mM | 0.1201 mL | 0.6007 mL | 1.2014 mL | |
| 10 mM | 0.0601 mL | 0.3003 mL | 0.6007 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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