Compstatin

Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.

Product information

CAS Number: 206645-99-0

Molecular Weight: 1550.77

Formula: C66H99N23O17S2

Chemical Name: 2-[(4R, 7S, 10S, 13S, 19S, 22S, 25S, 28S, 31S, 34R)-4-[[(2S, 3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-34-[[(2S, 3S)-2-amino-3-methylpentanoyl]amino]-25-(3-amino-3-oxopropyl)-7-[3-(diaminomethylideneamino)propyl]-10, 13-bis(1H-imidazol-5-ylmethyl)-19-(1H-indol-3-ylmethyl)-6, 9, 12, 15, 18, 21, 24, 27, 30, 33-decaoxo-28, 31-di(propan-2-yl)-1, 2-dithia-5, 8, 11, 14, 17, 20, 23, 26, 29, 32-decazacyclopentatriacont-22-yl]acetic acid

Smiles: CCC(C)C(N)C(=O)NC1CSSCC(NC(=O)C(CCCN=C(N)N)NC(=O)C(CC2=CN=CN2)NC(=O)C(CC2=CN=CN2)NC(=O)CNC(=O)C(CC2=CNC3=CC=CC=C23)NC(=O)C(CC(O)=O)NC(=O)C(CCC(N)=O)NC(=O)C(NC(=O)C(NC1=O)C(C)C)C(C)C)C(=O)NC(C(C)O)C(N)=O

InChiKey: RDTRHBCZFDCUPW-UHFFFAOYSA-N

InChi: InChI=1S/C66H99N23O17S2/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/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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Compstatin exhibits an in vitro half-life in human blood of about2 hr. In solution, compstatin forms a β-turn at residues Gln-5–Gly-8 with the disulfide bridge Cys-2–Cys12, residues Ile-1–Val-4, and Thr-13, forming a hydrophobic cluster.

In Vivo:

Compstatin (21 mg/kg) produces complete inhibition when given as a combination of bolus injection and infusion. 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. Compstatin is stable in baboon plasma for more than 24 h. Pig xenografts survival is significantly longer in the Compstatin perfused group than in the control group.

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.

Products are for research use only. Not for human use.