400-998-5282
专注多肽 服务科研

编号:110109
CAS号:100513-58-4/100915-92-2
单字母:H2N-YSEEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEII-CONH2
"Tyrosyl-CRF is a protein-based activator of the catecholamine receptor. It can be used as a research tool to study the function of the catecholamine receptor and ion channels, or as an inhibitor of these receptors. Tyrosyl-CRF binds to the alpha subunit of the catecholamine receptor. This binding causes conformational changes in the receptor that activate it when tyrosine residues are present in the cytoplasmic domain. Tyrosyl-CRF is also able to bind to other proteins such as peptides and antibodies, which may have therapeutic potential for use in diseases such as cancer, Alzheimers disease, and Parkinsons disease."
| DOI | 名称 | |
|---|---|---|
| 10.1016/s0014-2999(00)00412-x | Increased corticotropin-releasing factor concentrations in the bed nucleus of the stria terminalis of anhedonic rats | 下载 |
| 10.1016/s0006-8993(00)02759-1 | Influence of corticotrophin releasing factor on neuronal cell death in vitro and in vivo | 下载 |
| 10.1046/j.1471-4159.2002.00903.x | Reciprocal regulation of calcium dependent and calcium independent cyclic AMP hydrolysis by protein phosphorylation | 下载 |
| 10.1046/j.1471-4159.2003.01544.x | Corticotropin-releasing hormone induces proliferation and TNF-alpha release in cultured rat microglia via MAP kinase signalling pathways | 下载 |
| 10.1016/j.neuroscience.2004.11.040 | The corticotropin-releasing factor (CRF)-system and monoaminergic afferents in the central amygdala: investigations in different mouse strains and comparison with the rat | 下载 |
| 10.1016/j.chroma.2006.01.102 | Measurement of neuropeptides in clinical samples using chip-based immunoaffinity capillary electrophoresis | 下载 |
| 10.1096/fj.05-5315fje | Activation of corticotropin-releasing factor receptor-2 causes bronchorelaxation and inhibits pulmonary inflammation in mice | 下载 |
| 10.1677/JOE-08-0011 | Interferon-gamma inhibits cellular proliferation and ACTH production in corticotroph tumor cells through a novel janus kinases-signal transducer and activator of transcription 1/nuclear factor-kappa B inhibitory signaling pathway | 下载 |
| 10.1096/fj.09-131391 | Annexin A1 regulates hormone exocytosis through a mechanism involving actin reorganization | 下载 |
| 10.1016/0165-0173(90)90012-d | Physiological and behavioral responses to corticotropin-releasing factor administration: is CRF a mediator of anxiety or stress responses? | 下载 |
| 10.1089/adt.2009.0232 | Comparing label-free biosensors for pharmacological screening with cell-based functional assays | 下载 |
| 10.1152/ajpendo.00155.2011 | Opposite effects of serum- and glucocorticoid-regulated kinase-1 and glucocorticoids on POMC transcription and ACTH release | 下载 |
| 10.1016/j.psyneuen.2012.07.016 | Examining the role of endogenous orexins in hypothalamus-pituitary-adrenal axis endocrine function using transient dual orexin receptor antagonism in the rat | 下载 |
| 10.1523/JNEUROSCI.1445-13.2013 | NMDA receptor activation and calpain contribute to disruption of dendritic spines by the stress neuropeptide CRH | 下载 |
| 10.1113/jphysiol.2015.284471 | Large conductance Ca²⁺-activated K⁺ (BK) channels promote secretagogue-induced transition from spiking to bursting in murine anterior pituitary corticotrophs | 下载 |
| 10.1002/cne.23796 | Sociality and the telencephalic distribution of corticotrophin-releasing factor, urocortin 3, and binding sites for CRF type 1 and type 2 receptors: A comparative study of eusocial naked mole-rats and solitary Cape mole-rats | 下载 |
| 10.15252/embj.201488795 | The stress response neuropeptide CRF increases amyloid-β production by regulating γ-secretase activity | 下载 |
| 10.1111/jnc.13195 | Short-term modern life-like stress exacerbates Aβ-pathology and synapse loss in 3xTg-AD mice | 下载 |
| 10.1371/journal.pone.0147250 | Functional Impact of Corticotropin-Releasing Factor Exposure on Tau Phosphorylation and Axon Transport | 下载 |
| 10.1016/j.cmet.2016.04.017 | CRFR1 in AgRP Neurons Modulates Sympathetic Nervous System Activity to Adapt to Cold Stress and Fasting | 下载 |
| 10.1016/j.cell.2016.08.067 | A Cortical Circuit for Sexually Dimorphic Oxytocin-Dependent Anxiety Behaviors | 下载 |
| 10.1038/s41598-017-18401-y | Murine splenic B cells express corticotropin-releasing hormone receptor 2 that affect their viability during a stress response | 下载 |
| 10.1016/j.bbrc.2004.06.128 | A novel soluble protein factor with non-opioid dynorphin A-binding activity | 下载 |
| 10.1111/j.1365-2982.2005.00644.x | Divergent role for CRF1 and CRF2 receptors in the modulation of visceral pain | 下载 |
| 10.1113/jphysiol.2007.150078 | Corticotropin-releasing factor increases mouse ventral tegmental area dopamine neuron firing through a protein kinase C-dependent enhancement of Ih | 下载 |
多肽H2N-Tyr-Ser-Glu-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Met-Glu-Ile-Ile-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1.08g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0.97mmol Fmoc-Ile-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1.94mmol DIPEA,0.92mmol 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-Ile-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-Ile-Linker-MBHA Resin
Fmoc-Ile-Ile-Linker-MBHA Resin
H2N-Ile-Ile-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Glu(OtBu)-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Glu(OtBu)-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Glu(OtBu)-Glu(OtBu)-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Ser(tBu)-Glu(OtBu)-Glu(OtBu)-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
H2N-Ser(tBu)-Glu(OtBu)-Glu(OtBu)-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Ser(tBu)-Glu(OtBu)-Glu(OtBu)-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-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)-Ser(tBu)-Glu(OtBu)-Glu(OtBu)-Pro-Pro-Ile-Ser(tBu)-Leu-Asp(OtBu)-Leu-Thr(tBu)-Phe-His(Trt)-Leu-Leu-Arg(Pbf)-Glu(OtBu)-Val-Leu-Glu(OtBu)-Met-Ala-Arg(Pbf)-Ala-Glu(OtBu)-Gln(Trt)-Leu-Ala-Gln(Trt)-Gln(Trt)-Ala-His(Trt)-Ser(tBu)-Asn(Trt)-Arg(Pbf)-Lys(Boc)-Leu-Met-Glu(OtBu)-Ile-Ile-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-Ser-Glu-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Met-Glu-Ile-Ile-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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