400-998-5282
专注多肽 服务科研

这种 NPY 类似物是不同细胞系和组织中 Y₁ 受体的高效选择性配体。因此,它已被用于检测 NPY/PYY 受体亚型分布,例如,在大鼠脑中。该肽在体内也具有活性,在增加麻醉大鼠的血压方面显示出比 NPY 更高的效力。
编号:155483
CAS号:125580-28-1
单字母:H2N-YPSKPDNPGEDAPAEDLARYYSALRHYINLLTRPRY-CONH2
这种 NPY 类似物是不同细胞系和组织中 Y₁ 受体的高效选择性配体。因此,它已被用于检测 NPY/PYY 受体亚型分布,例如,在大鼠脑中。该肽在体内也具有活性,在增加麻醉大鼠的血压方面显示出比 NPY 更高的效力。
This NPY analog is a highly potent and selective ligand for Y₁ receptors in different cell lines and tissues. It has therefore been used to detect the NPY/PYY receptor subtype distribution, e.g., in rat brain. The peptide is also active in vivo, showing an even higher potency than NPY in increasing blood pressure in anesthetized rats.
[Leu31,Pro34]-神经肽Y(猪)是一种高亲和力神经肽Y Y1受体激动剂(Ki=0.54nM)。
[Leu31,Pro34]-Neuropeptide Y (porcine) is a high affinity neuropeptide Y Y1 receptor agonist (Ki = 0.54 nM).
NPY is a neuropeptide that belongs to the peptide family of neuropeptides. NPY is an activator of G-protein coupled receptors, and it regulates a variety of physiological functions, such as feeding behavior, energy expenditure and water balance. NPY is also involved in various diseases, such as diabetes mellitus, hypertension and cardiac hypertrophy. NPY (Porcine) can be used as a research tool for studying the biological function of NPY or for ligand-binding assays.
亮氨酸 ³¹, 脯氨酸 ³⁴ 神经肽 Y(1-36)(猪)具有调节 C 端区域折叠的取代,该区域对受体特异性很重要。该肽支持跨物种结构比较。其序列有助于研究神经肽 - 蛋白质相互作用和构象转变。应用包括肽工程和受体结合研究。
Leu31,Pro34 Neuropeptide Y (1-36), porcine features substitutions that modulate folding in the C-terminal region important for receptor specificity. The peptide supports structural comparison across species. Its sequence aids in studying neuropeptide-protein interaction and conformational transitions. Applications include peptide engineering and receptor-binding research.
Leu31,Pro34‑猪神经肽 Y 是一种 NPY 修饰类似物,残基可影响主链刚性与受体结合研究。脯氨酸引入构象限制,亮氨酸增强疏水作用。用于神经肽基序特异性研究。
Leu31,Pro34-Neuropeptide Y (porcine) is a modified NPY analog featuring residues that influence backbone rigidity and receptor-binding studies. Proline introduces conformational constraints, while leucine enhances hydrophobic interactions. The sequence supports structural mapping. Researchers apply it in motif-specific neuropeptide research.
| DOI | 名称 | |
|---|---|---|
| 10.1046/j.0014-2956.2001.02561.x | A neuropeptide Y receptor Y1-subfamily gene from an agnathan, the European river lamprey. A potential ancestral gene | 下载 |
| 10.1046/j.1471-4159.2002.00817.x | Pharmacological characterization of cloned chicken neuropeptide Y receptors Y1 and Y5 | 下载 |
| 10.1016/0197-0186(92)90067-2 | [Leu31-Pro34] neuropeptide Y identifies a subtype of 125I-labeled peptide YY binding sites in the rat brain | 下载 |
| 10.1073/pnas.87.1.182 | [Leu31, Pro34]neuropeptide Y: a specific Y1 receptor agonist | 下载 |
| 10.1111/j.1471-4159.2011.07541.x | Neuropeptide Y inhibits interleukin-1 beta-induced microglia motility | 下载 |
| 10.1186/1742-2094-8-169 | Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells | 下载 |
| 10.4303/jdar/235604 | Contrasting Effects of the Neuropeptides Substance P, Somatostatin, and Neuropeptide Y on the Methamphetamine-Induced Production of Striatal Nitric Oxide in Mice | 下载 |
多肽H2N-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro-Ala-Glu-Asp-Leu-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Leu-Thr-Arg-Pro-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2.09g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1.88mmol 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3.76mmol DIPEA,1.79mmol 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-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Lys(Boc)-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Lys(Boc)-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ser(tBu)-Lys(Boc)-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ser(tBu)-Lys(Boc)-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Ser(tBu)-Lys(Boc)-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Ser(tBu)-Lys(Boc)-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Pro-Ser(tBu)-Lys(Boc)-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-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-Tyr(tBu)-Pro-Ser(tBu)-Lys(Boc)-Pro-Asp(OtBu)-Asn(Trt)-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Pro-Ala-Glu(OtBu)-Asp(OtBu)-Leu-Ala-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ser(tBu)-Ala-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Ile-Asn(Trt)-Leu-Leu-Thr(tBu)-Arg(Pbf)-Pro-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-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro-Ala-Glu-Asp-Leu-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Leu-Thr-Arg-Pro-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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