艾卡拉肽 | 460738-38-9

• 物质功能分类: 生物化工 - 多肽
• 分子结构分类: 有机化合物 - 有机聚合物 - 多肽
• 中文名称: 艾卡拉肽
• 英文名称: H-Glu-Ala-Met-D-His-D-Ser-Phe-Cys(1)-D-Ala-Phe-D-Lys-Ala-D-Asp-D-Asp-Gly-D-Pro-Cys(2)-D-Arg-D-Ala-D-Ala-D-His-D-Pro-D-Arg-D-Trp-D-Phe-D-Phe-Asn-D-Ile-Phe-D-aThr-D-Arg-D-Gln-Cys(3)-Glu-Glu-Phe-aIle-D-Tyr-Gly-Gly-Cys(2)-D-Glu-Gly-D-Asn-Gln-Asn-Arg-Phe-Glu-Ser-Leu-Glu-Glu-Cys(3)-D-Lys-D-Lys-D-Met-Cys(1)-aThr-Arg-D-Asp-OH
• 英文别名: (2R)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4R,5aS,8aS,11aR,13R,14aR,16R,17aR,19S,20aR,22R,23aS,25S,26aR,28R,29aS,31R,32aR,35aR,36R,38aR,39R,41aR,42R,44aR,45R,48R,50aR,51S,53aR,54S,56aR,57S,59aR,60S,63S,66S,69S,72S,75S,78R,84R,87R,96R,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2R)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1R)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid
• CAS: 460738-38-9
• 化学式: C₃₀₅H₄₄₂N₈₈O₉₁S₈
• 分子量: 7054.0
• InChiKey: VBGWSQKGUZHFPS-BRUBJIIKSA-N

制备方法与用途

用途

艾卡拉肽（商品名：Kalbitor）用于遗传性血管水肿（HAE）突发或致命性积液的治疗。艾卡拉肽是在美国上市的第二种治疗HAE发作的药物。

制备

将150g艾卡拉肽线性粗肽溶解于150L的缓冲体系中，该缓冲体 系为0.1mM醋酸铵、3倍量于线性粗肽(物质的量)的DTT的水溶液， pH为7.8，敞口置于室温中，搅拌36小时，加冰乙酸调节pH=3～5淬 灭，即得到艾卡拉肽粗肽溶液，并参照实施例12的方法进行纯化制备 并冻干，得到白色精肽固体35.7g，环化收率为23.8%，质谱信号为 8387.654。