Al-18F mark fusion peptide and application thereof
A label fusion, al-18f technology, applied in the biological field, can solve the problems of pharmaceutical, inconvenient transportation, increased use cost, clinical application obstacles, etc., to improve probe concentration, improve specificity, and improve target/non-target The effect of target ratio
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[0035] Example 1
[0036] (1) Preparation of NOTA-PEG-RGDyK-Lys-Ac-A7R:
[0037] The reaction formula is as follows:
[0038]
[0039] Specifically: RGDyK-Lys-Ac-A7R can be purchased at home and abroad (Hangzhou Zhongpi Biochemical Co., Ltd.). Dissolve [2-[2-(fluorenylmethoxycarbonyl-amino)ethoxy]ethoxy]acetic acid in 1mL DMF (dimethylformamide), add NHS (N-hydroxysuccinimide, also called For HOSU) and DCC (bicyclohexyl carbodiimide), the reaction was stirred at room temperature for 2 hours. Add RGDyK-Lys-Ac-A7R to the above reaction solution, adjust the pH to 8.0-8.5 with DIEA (N,N-diisopropylethylamine), and stir at room temperature overnight. Add 3 mL of 0.5M NH4OAc buffer (pH=7.0) to the reaction solution and filter. The filtrate is separated and purified by HPLC. The fractions of the target product are collected, combined and lyophilized. The product is fluorenylmethoxycarbonyl-PEG-RGDyK-Lys-Ac- A7R adds 20% piperidine and reacts at room temperature for 30 minutes to remove ...
Example Embodiment
[0047] Example 2
[0048] This example is a comparative example, and the comparative object is [Al 18 F]NOTA-PEG-RGDyK, the structural formula is as follows:
[0049]
[0050] The preparation method is as follows:
[0051] (1) RGDyK can be purchased at home and abroad. Dissolve [2-[2-(fluorenylmethoxycarbonyl-amino)ethoxy]ethoxy]acetic acid in 1mL DMF (dimethylformamide), add NHS (N-hydroxysuccinimide, also called For HOSU) and DCC (bicyclohexyl carbodiimide), the reaction was stirred at room temperature for 2 hours. Add RGDyK to the above reaction solution, adjust the pH to 8.0-8.5 with DIEA (N,N-diisopropylethylamine), and stir at room temperature overnight. Add 3mL 0.5M NH4OAc buffer (pH=7.0) to the reaction solution and filter. The filtrate is separated and purified by HPLC. The fractions of the target product are collected, combined and lyophilized. The product fluorenylmethoxycarbonyl-PEG-RGDyK is added with 20% piperidine React at room temperature for 30 minutes to remove ...
Example Embodiment
[0056] Example 3
[0057] This example is a comparative example, and the comparative object is [Al 18 F]NOTA-PEG3-A7R, the structural formula is as follows:
[0058]
[0059] (1) A7R can be purchased at home and abroad. Dissolve [2-[2-(fluorenylmethoxycarbonyl-amino)ethoxy]ethoxy]acetic acid in 1mL DMF (dimethylformamide), add NHS (N-hydroxysuccinimide, also called For HOSU) and DCC (bicyclohexyl carbodiimide), the reaction was stirred at room temperature for 2 hours. Add ATWLPPR to the above reaction solution, adjust the pH to 8.0-8.5 with DIEA (N,N-diisopropylethylamine), and stir at room temperature overnight. Add 3mL 0.5M NH4OAc buffer (pH=7.0) to the reaction solution and filter. The filtrate is separated and purified by HPLC. The fractions of the target product are collected, combined and freeze-dried. The product fluorenylmethoxycarbonyl-PEG-A7R is added with 20% piperidine React at room temperature for 30 minutes to remove the fluorenylmethyloxycarbonyl group, and then a...
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