Compstatin

製品コードS8522 バッチS852201

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₆₆H₉₉N₂₃O₁₇S₂
	分子量	1550.77	CAS No.	206645-99-0
Solubility (25°C)*	体外	Water	100 mg/mL (64.48 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Compstatin binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.
in vitro	Compstatin binds to native C3 and inhibits its cleavage by C3 convertase. Binding of Compstatin to native C3 is a multistep reaction that is preferred over its binding to the C3 fragments C3b and C3c. N-acetylation of Compstatin provides stability against enzymatic degradation^[1]. Compstatin features a high selectivity for human and primate C3. While binding to C3 from baboons and other primates shows comparable interaction profiles as its human counterpart, no binding is detected for C3 from lower mammalian species such as mice, rats, guinea pigs, rabbits, or pigs^[3].
in vivo	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 a safe and effective complement inhibitor that has the potential to prevent complement activation during and after clinical cardiac surgery. Furthermore, Compstatin can serve as the prototype for designing an orally administrated drug. In the extracorporeal circulation model, Compstatin inhibits the generation of C3a and C5a, the formation of the membrane attack complex, and CD11b expression on neutrophils (PMNs). The peptide also inhibits binding of C3/C3 fragments, PMNs, and monocytes to the polymer surface^[2].

製品説明

Compstatin binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.

in vitro

Compstatin binds to native C3 and inhibits its cleavage by C3 convertase. Binding of Compstatin to native C3 is a multistep reaction that is preferred over its binding to the C3 fragments C3b and C3c. N-acetylation of Compstatin provides stability against enzymatic degradation^[1].

Compstatin features a high selectivity for human and primate C3. While binding to C3 from baboons and other primates shows comparable interaction profiles as its human counterpart, no binding is detected for C3 from lower mammalian species such as mice, rats, guinea pigs, rabbits, or pigs^[3].

in vivo

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 a safe and effective complement inhibitor that has the potential to prevent complement activation during and after clinical cardiac surgery. Furthermore, Compstatin can serve as the prototype for designing an orally administrated drug. In the extracorporeal circulation model, Compstatin inhibits the generation of C3a and C5a, the formation of the membrane attack complex, and CD11b expression on neutrophils (PMNs). The peptide also inhibits binding of C3/C3 fragments, PMNs, and monocytes to the polymer surface^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	iPSC-ECs
	濃度	50 μM
	反応時間	2 days
	実験の流れ	Cells were treated with indicated concentration of drug for 2 days.
動物実験	動物モデル	Juvenile baboons (P. anubis)
	投薬量	17, 21, 34, 38.5, 50, 63.5 mg/kg
	投与方法	by bolus injection, infusion, or both

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Peptidoglycan from Bacillus anthracis Inhibits Human Macrophage Efferocytosis in Part by Reducing Cell Surface Expression of MERTK and TIM-3 [ bioRxiv, 2023, 2023.03.30.535001]	PubMed: 37066181
Low molecular weight polysialic acid binds to properdin and reduces the activity of the alternative complement pathway [ Sci Rep, 2022, 12(1):5818]	PubMed: 35388026
Patient-specific iPSC-derived endothelial cells reveal aberrant p38 MAPK signaling in atypical hemolytic uremic syndrome [ Stem Cell Reports, 2021, 16(9):2305-2319]	PubMed: 34388364

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。