A peptide inhibitor of complement activation
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Compstatin (trifluoroacetate salt)

Item No. 34435

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
L-isoleucyl-L-cysteinyl-L-valyl-L-valyl-L-glutaminyl-L-α-aspartyl-L-tryptophylglycyl-L-histidyl-L-histidyl-L-arginyl-L-cysteinyl-L-threoninamide, cyclic (2→12)-disulfide, trifluoroacetate salt
Synonyms
  • ICVVQDWGHHRCT
Molecular Formula
C66H99N23O17S2 • XCF3COOH
Formula Weight
1550.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 10 mg/mlEthanol: slightly solublePBS (pH 7.2): 10 mg/ml
λmax
220 nm
SMILES
O=C([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](CSSC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC1=O)=O)CC2=CN=CN2)=O)CC3=CN=CN3)=O)CCCNC(N)=N)=O)C(N[C@H]([C@@H](C)O)C(N)=O)=O)NC([C@@H](N)[C@@H](C)CC)=O)=O)C(C)C)=O)C(C)C)=O)CCC(N)=O)=O)CC(O)=O)N[C@H]1CC4=CNC5=CC=CC=C45.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C66H99N23O17S2.C2HF3O2/c1-8-32(6)50(68)63(104)86-46-27-108-107-26-45(62(103)89-53(33(7)90)54(69)95)85-56(97)39(14-11-17-74-66(70)71)80-59(100)43(20-36-24-73-29-78-36)83-58(99)42(19-35-23-72-28-77-35)79-48(92)25-76-55(96)41(18-34-22-75-38-13-10-9-12-37(34)38)82-60(101)44(21-49(93)94)84-57(98)40(15-16-47(67)91)81-64(105)51(30(2)3)88-65(106)52(31(4)5)87-61(46)102;3-2(4,5)1(6)7/h9-10,12-13,22-24,28-33,39-46,50-53,75,90H,8,11,14-21,25-27,68H2,1-7H3,(H2,67,91)(H2,69,95)(H,72,77)(H,73,78)(H,76,96)(H,79,92)(H,80,100)(H,81,105)(H,82,101)(H,83,99)(H,84,98)(H,85,97)(H,86,104)(H,87,102)(H,88,106)(H,89,103)(H,93,94)(H4,70,71,74);(H,6,7)/t32-,33+,39-,40-,41-,42-,43-,44-,45-,46-,50-,51-,52-,53+;/m0./s1
InChi Key
DURMUHTUCAQKNL-CJVVNLCASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Compstatin is a cyclic peptide inhibitor of complement activation (IC50s = 63 and 12 µM for the classical and alternative pathways, respectively).1,2 It binds to complement component 3 (C3) and inhibits convertase-mediated cleavage of C3 to the complement activation products C3a and C3b.3 Compstatin (70 µM) inhibits the generation of C3a, activation of polymorphonuclear leukocytes (PMNs), and the binding of PMNs to the polymer surface in an isolated human whole blood model of extracorporeal circulation.4 In vivo, compstatin (21 mg/kg) inhibits the generation of C3b, C3c, and iC3b in a baboon model of heparin- and protamine-induced complement activation.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sahu, A., Kay, B.K., and Lambris, J.D. Inhibition of human complement by a C3-binding peptide isolated from a phage-displayed random peptide library. J. Immunol. 157(2), 884-891 (1996).

    2. Huang, Y. Evolution of compstatin family as therapeutic complement inhibitors. Expert Opin. Drug Discov. 13(5), 435-444 (2018).

    3. Ricklin, D., and Lambris, J.D. Compstatin: A complement inhibitor on its way to clinical application. Adv. Exp. Med. Biol. 632, 273-292 (2008).

    4. Nilsson, B., Larsson, R., Hong, J., et al. Compstatin inhibits complement and cellular activation in whole blood in two models of extracorporeal circulation. Blood 92(5), 1661-1667 (1998).

    5. Soulika, A.M., Khan, M.M., Hattori, T., et al. Inhibition of heparin/protamine complex-induced complement activation by Compstatin in baboons. Clin. Immunol. 96(3), 212-221 (2000).