Compstatin TFA 是一个 13 残基环肽,是补体系统C3的有效抑制剂,具有物种特异性。Compstatin TFA 结合到狒狒的 C3,并对狒狒血液中的蛋白水解裂解具有抗性 (类似人类)。Compstatin TFA 只抑制灵长类补体系统的激活。Compstatin TFA 对补体经典途径和旁路途径的 IC50值分别为 63 μM 和 12 μM。
生物活性 | Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of thecomplement systemC3with 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 IC50values of 63 μM and 12 μM for classical and alterative complement pathway, respectively[1][2][3]. |
体外研究 (In Vitro) | 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].
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体内研究 (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[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].
Animal Model: | Juvenile baboons (P. Anubis) weighing 10.5-28.8 kg[1]. | Dosage: | 50, 25 mg/kg 60 min after heparin and 2 min before protamine. | Administration: | A bolus injection. | Result: | Completely inhibited complement activation induced by heparin–protamine complexes. |
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分子量 | |
性状 | |
Formula | |
Sequence Shortening | ICVVQDWGHHRCT-NH2 (Disulfide bridge: Cys2-Cys12) |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Protect from light, stored under nitrogen Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : 110 mg/mL(66.07 mM;Need ultrasonic) H2O : 50 mg/mL(30.03 mM;Need ultrasonic) 配制储备液 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 |
*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℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 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。 *以上所有助溶剂都可在本网站选购。
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