这种含有 (Ala-Aib) 的胰肽/神经肽 Y 嵌合体是一种高度选择性的神经肽 Y₅ 受体激动剂。在该受体上，该化合物的效力比衍生物 (Ala³¹,Aib³²)-pNPY（0.24 nM 对 6 nM）强 25 倍，比天然配体神经肽 Y（0.24 nM 对 0.6 nM）强三倍,.,事实证明，这种类似物增加喂养的效果比神经肽 Y 高约 2.5 倍。
编号：200285
CAS号：313988-89-5
单字母：H2N-GPSQPTYPGDNATPEQMARYYSALRRYINMA-Aib-RQRY-CONH2
| 编号: | 200285 |
| 中文名称: | 神经肽Gly1,Gln4·16,Thr6·13,Tyr7,Asp10,Asn11,Pro14,Arg |
| 英文名: | (Gly1,Gln4·16,Thr6·13,Tyr7,Asp10,Asn11,Pro14,Arg26 |
| CAS号: | 313988-89-5 |
| 单字母: | H2N-GPSQPTYPGDNATPEQMARYYSALRRYINMA-Aib-RQRY-CONH2 |
| 三字母: | H2N N端氨基 -Gly甘氨酸 -Pro脯氨酸 -Ser丝氨酸 -Gln谷氨酰胺 -Pro脯氨酸 -Thr苏氨酸 -Tyr酪氨酸 -Pro脯氨酸 -Gly甘氨酸 -Asp天冬氨酸 -Asn天冬酰胺 -Ala丙氨酸 -Thr苏氨酸 -Pro脯氨酸 -Glu谷氨酸 -Gln谷氨酰胺 -Met甲硫氨酸 -Ala丙氨酸 -Arg精氨酸 -Tyr酪氨酸 -Tyr酪氨酸 -Ser丝氨酸 -Ala丙氨酸 -Leu亮氨酸 -Arg精氨酸 -Arg精氨酸 -Tyr酪氨酸 -Ile异亮氨酸 -Asn天冬酰胺 -Met甲硫氨酸 -Ala丙氨酸 -Aib暂无说明 -Arg精氨酸 -Gln谷氨酰胺 -Arg精氨酸 -Tyr酪氨酸 -CONH2C端酰胺化 |
| 氨基酸个数: | 36 |
| 分子式: | C183H281N57O54S2 |
| 平均分子量: | 4207.67 |
| 精确分子量: | 4205.04 |
| 等电点(PI): | 12.69 |
| pH=7.0时的净电荷数: | 8.97 |
| 平均亲水性: | -0.11724137931034 |
| 疏水性值: | -1.21 |
| 消光系数: | 7450 |
| 来源: | 人工化学合成，仅限科学研究使用，不得用于人体。 |
| 储存条件: | 负80℃至负20℃ |
| 标签: | 氨基酸衍生物肽 |
This (Ala-Aib)-containing pancreatic peptide/neuropeptide Y chimera is a highly selective neuropeptide Y₅ receptor agonist. At this receptor this compound turned out to be 25-fold more potent than the derivative (Ala³¹,Aib³²)-pNPY (0.24 nM vs 6 nM) and three-fold more potent than the native ligand neuropeptide Y (0.24 nM vs 0.6 nM). This analog turned out to increase feeding approximately 2.5-fold more effective than neuropeptide Y.
| DOI | 名称 | |
|---|---|---|
| 10.1111/j.1471-4159.2004.03005.x | Up-regulation of neuropeptide Y levels and modulation of glutamate release through neuropeptide Y receptors in the hippocampus of kainate-induced epileptic rats | 下载 |
| 10.1111/j.1471-4159.2008.05334.x | Neuropeptide Y stimulates retinal neural cell proliferation--involvement of nitric oxide | 下载 |
| 10.1016/j.neuropharm.2012.02.015 | Neuropeptide Y promotes neurogenesis and protection against methamphetamine-induced toxicity in mouse dentate gyrus-derived neurosphere cultures | 下载 |
| 10.1038/cddis.2013.160 | Neuropeptide Y receptors activation protects rat retinal neural cells against necrotic and apoptotic cell death induced by glutamate | 下载 |
多肽H2N-Gly-Pro-Ser-Gln-Pro-Thr-Tyr-Pro-Gly-Asp-Asn-Ala-Thr-Pro-Glu-Gln-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-Arg-Tyr-Ile-Asn-Met-Ala-Aib-Arg-Gln-Arg-Tyr-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1.82g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1.64mmol Fmoc-Tyr(tBu)-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3.28mmol DIPEA，1.56mmol 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-Tyr(tBu)-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-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Gln(Trt)-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Gln(Trt)-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ser(tBu)-Gln(Trt)-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ser(tBu)-Gln(Trt)-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Ser(tBu)-Gln(Trt)-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Ser(tBu)-Gln(Trt)-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Gly-Pro-Ser(tBu)-Gln(Trt)-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-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-Gly-Pro-Ser(tBu)-Gln(Trt)-Pro-Thr(tBu)-Tyr(tBu)-Pro-Gly-Asp(OtBu)-Asn(Trt)-Ala-Thr(tBu)-Pro-Glu(OtBu)-Gln(Trt)-Met-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-Arg(Pbf)-Tyr(tBu)-Ile-Asn(Trt)-Met-Ala-Aib-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-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-Gly-Pro-Ser-Gln-Pro-Thr-Tyr-Pro-Gly-Asp-Asn-Ala-Thr-Pro-Glu-Gln-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-Arg-Tyr-Ile-Asn-Met-Ala-Aib-Arg-Gln-Arg-Tyr-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。
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