Compstatinis is a 13-residue cyclic peptide, binds to complement component C3 and inhibits complement activation with IC50 of 12 μM. Compstatin features a high selectivity for human and primate C3. Compstatin completely inhibits in vivo heparin/protamine-induced complement activation without adverse effects on heart rate or systemic arterial, central venous, and pulmonary arterial pressures.
|Animal models||Juvenile baboons (P. anubis)|
|Dosages||17, 21, 34, 38.5, 50, 63.5 mg/kg|
|Administration||by bolus injection, infusion, or both|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||Water ≥ 90 mg/mL|
Compstatin: a C3-targeted complement inhibitor reaching its prime for bedside intervention.
Mastellos DC, et al. Eur J Clin Invest. 2015 Apr;45(4):423-40. PMID: 25678219.
Inhibition of heparin/protamine complex-induced complement activation by Compstatin in baboons.
Soulika AM, et al. Clin Immunol. 2000 Sep;96(3):212-21. PMID: 10964539.
Binding kinetics, structure-activity relationship, and biotransformation of the complement inhibitor compstatin.
Sahu A, et al. J Immunol. 2000 Sep 1;165(5):2491-9. PMID: 10946275.
Compstatin, a peptide inhibitor of C3, prolongs survival of ex vivo perfused pig xenografts.
Fiane AE, et al. Xenotransplantation. 1999 Feb;6(1):52-65. PMID: 10355733.
Phytohemagglutinin is a lectin obtained from the red kidney bean that binds to the membranes of T-cells, stimulates metabolic activity and involves inflammatory pathways.
Apilimod is a potent IL-12/IL-23 inhibitor, and it is also a cell permeable small molecule which specifically inhibits PIKfyve with an IC50 of 14 nM in an in vitro kinase assay.
10-Hydroxy-trans-2-decenoic acid is the principal lipid component in royal jelly which is the food for queen and larvae honeybees.
Brij-35 (Polidocanol) is a high HLB, ethoxylated, nonionic ether of lauryl alcohol with broad pH stability.
Hyaluronic acid (HA) is an anionic, nonsulfated glycosaminoglycan distributed widely throughout connective, epithelial, and neural tissues.
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