Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively^[1][2][3].

Compstatin exhibits an in vitro half-life in human blood of about 2 hr^[2].
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^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].
Compstatin is stable in baboon plasma for more than 24 h^[1].
Pig xenografts survival is significantly longer in the Compstatin perfused group than in the control group^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1664.79

C₆₈H₁₀₀F₃N₂₃O₁₉S₂

ICVVQDWGHHRCT-NH2 (Disulfide bridge: Cys2-Cys12)

Room temperature in continental US; may vary elsewhere.

Protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

DMSO : 110 mg/mL (66.07 mM; Need ultrasonic)

H₂O : 50 mg/mL (30.03 mM; Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

  Solubility: ≥ 2.75 mg/mL (1.65 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (1.65 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.75 mg/mL (1.65 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (1.65 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

  Solubility: ≥ 2.75 mg/mL (1.65 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (1.65 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.