400-998-5282
专注多肽 服务科研

一种有效的 PACAP 受体拮抗剂。
编号:141018
CAS号:143748-18-9
单字母:H2N-FTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK-CONH2
| 参考文献(References): | P. Robberecht et al., Mol. Pharmacol., 42, 347 (1992) P. Robberecht et al., Eur. J. Biochem., 207, 239 (1992) F. Ohno et al., Regul. Peptides, 126, 115 (2005) P. Robberecht, P. Gourlet, P. De Neef, M-C. Woussen-Colle, M-C. Vandermeers-Piret,A. Vandermeers, and J. Christophe, Eur. J. Biochem., 207, 239 (1992) (Original) A. Vandermeers, S. Vandenborre, X. Hou, P. De Neef, P. Robberecht, M-C. Vandermeers-Piret,and J. Christophe, Eur. J. Biochem., 208, 815 (1992) (Pharmacol.) |
PACAP (6-38), human, ovine, rat 是一种有效的 PACAP 受体拮抗剂。PACAP (6-38) 作用于 PACAP I 型受体,PACAP II 型受体 VIP1 和 PACAP II 型受体 VIP2,IC50 分别为 30 nM,600 nM 和 40 nM。
PACAP (6-38), human, ovine, rat is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively.
PACAP是一种属于激活剂类别的肽。它被用作研究工具,因为它能够激活哺乳动物细胞中的离子通道。PACAP与受体相互作用,可以在中枢神经系统和外周组织中发现。PACAP的受体称为PAC1受体,与G蛋白偶联并调节腺苷酸环化酶活性。已显示PACAP在各种类型的癌细胞中抑制细胞增殖并促进细胞凋亡。\nPACAP还刺激神经垂体细胞释放催产素,这可能导致其用于治疗自闭症谱系障碍或抑郁症。
PACAP is a peptide that belongs to the class of activators. It is used as a research tool for its ability to activate ion channels in mammalian cells. PACAP interacts with receptors and can be found in both the central nervous system and peripheral tissues. The receptor for PACAP, known as the PAC1 receptor, is coupled to G-proteins and regulates adenylate cyclase activity. PACAP has been shown to inhibit cell proliferation and promote apoptosis in various types of cancer cells.\nPACAP also stimulates the release of oxytocin from neurohypophysis cells, which may lead to its use as a treatment for autism spectrum disorders or depression.
该肽是PACAP的片段6-38,它是PACAP-27刺激的垂体腺苷酸环化酶比PACAP(6-27)更有效和选择性的抑制剂。抑制酶的Ki值分别为7 nM和150 nM。
This peptide is the fragment 6-38 of PACAP, which is a much more potent and selective inhibitor of PACAP-27-stimulated pituitary adenylate cyclase than PACAP (6-27). Ki values for the inhibition of the enzyme were 7 nM and 150 nM respectively.
PACAP-38(6-38)(人、鸡、小鼠、羊、猪、大鼠)代表全长肽的主要部分,保留功能性螺旋结构域。序列保守性能够进行比较生物分析。构象特征支持受体结合研究。该片段经常用于结构 - 功能研究。
PACAP-38 (6-38) (human, chicken, mouse, ovine, porcine, rat) represents a major portion of the full-length peptide, retaining functional helical domains. Sequence conservation enables comparative biological analysis. Conformational characteristics support receptor-binding studies. The fragment is frequently used in structure–function investigations.
| DOI | 名称 | |
|---|---|---|
| 10.1016/j.neulet.2007.08.037 | Changes of dopamine content and cell proliferation by dexamethsone via pituitary adenylate cyclase-activating polypeptide in PC12 cell | 下载 |
| 10.1007/s12031-016-0764-1 | Intravesical PAC1 Receptor Antagonist, PACAP(6-38), Reduces Urinary Bladder Frequency and Pelvic Sensitivity in NGF-OE Mice | 下载 |
| 10.1016/0014-2999(95)00467-5 | Fragments of pituitary adenylate cyclase activating polypeptide discriminate between type I and II recombinant receptors | 下载 |
多肽H2N-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys-NH2的合成步骤:
1、合成MBHA树脂:取若干克的MBHA树脂(如初始取代度为0.5mmol/g)和1倍树脂摩尔量的Fmoc-Linker-OH加入到反应器中,加入DMF,搅拌使氨基酸完全溶解。再加入树脂2倍量的DIEPA,搅拌混合均匀。再加入树脂0.95倍量的HBTU,搅拌混合均匀。反应3-4小时后,用DMF洗涤3次。用2倍树脂体积的10%乙酸酐/DMF 进行封端30分钟。然后再用DMF洗涤3次,甲醇洗涤2次,DCM洗涤2次,再用甲醇洗涤2次。真空干燥12小时以上,得到干燥的树脂{Fmoc-Linker-MHBA Resin},测定取代度。这里测得取代度为 0.3mmol/g。结构如下图:

2、脱Fmoc:取2.76g的上述树脂,用DCM或DMF溶胀20分钟。用DMF洗涤2遍。加3倍树脂体积的20%Pip/DMF溶液,鼓氮气30分钟,然后2倍树脂体积的DMF 洗涤5次。得到 H2N-Linker-MBHA Resin 。(此步骤脱除Fmoc基团,茚三酮检测为蓝色,Pip为哌啶)。结构图如下:

3、缩合:取2.48mmol Fmoc-Lys(Boc)-OH 氨基酸,加入到上述树脂里,加适当DMF溶解氨基酸,再依次加入4.97mmol DIPEA,2.36mmol HBTU。反应30分钟后,取小样洗涤,茚三酮检测为无色。用2倍树脂体积的DMF 洗涤3次树脂。(洗涤树脂,去掉残留溶剂,为下一步反应做准备)。得到Fmoc-Lys(Boc)-Linker-MBHA Resin。氨基酸:DIPEA:HBTU:树脂=3:6:2.85:1(摩尔比)。结构图如下:

4、依次循环步骤二、步骤三,依次得到
H2N-Lys(Boc)-Linker-MBHA Resin
Fmoc-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
H2N-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
Fmoc-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin
以上中间结构,均可在专肽生物多肽计算器-多肽结构计算器中,一键画出。
最后再经过步骤二得到 H2N-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Gly-Lys(Boc)-Arg(Pbf)-Tyr(tBu)-Lys(Boc)-Gln(Trt)-Arg(Pbf)-Val-Lys(Boc)-Asn(Trt)-Lys(Boc)-Linker-MBHA Resin,结构如下:

5、切割:6倍树脂体积的切割液(或每1g树脂加8ml左右的切割液),摇床摇晃 2小时,过滤掉树脂,用冰无水乙醚沉淀滤液,并用冰无水乙醚洗涤沉淀物3次,最后将沉淀物放真空干燥釜中,常温干燥24小试,得到粗品H2N-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys-NH2。结构图见产品结构图。
切割液选择:1)TFA:H2O=95%:5%
2)TFA:H2O:TIS=95%:2.5%:2.5%
3)三氟乙酸:茴香硫醚:1,2-乙二硫醇:苯酚:水=87.5%:5%:2.5%:2.5%:2.5%
(前两种适合没有容易氧化的氨基酸,例如Trp、Cys、Met。第三种适合几乎所有的序列。)
6、纯化冻干:使用液相色谱纯化,收集目标峰液体,进行冻干,获得蓬松的粉末状固体多肽。不过这时要取小样复测下纯度 是否目标纯度。
7、最后总结:
杭州专肽生物技术有限公司(ALLPEPTIDE https://www.allpeptide.com)主营定制多肽合成业务,提供各类长肽,短肽,环肽,提供各类修饰肽,如:荧光标记修饰(CY3、CY5、CY5.5、CY7、FAM、FITC、Rhodamine B、TAMRA等),功能基团修饰肽(叠氮、炔基、DBCO、DOTA、NOTA等),同位素标记肽(N15、C13),订书肽(Stapled Peptide),脂肪酸修饰肽(Pal、Myr、Ste),磷酸化修饰肽(P-Ser、P-Thr、P-Tyr),环肽(酰胺键环肽、一对或者多对二硫键环),生物素标记肽,PEG修饰肽,甲基化修饰肽等。
以上所有内容,为专肽生物原创内容,请勿发布到其他网站上。





