400-998-5282
专注多肽 服务科研

胃抑制素(GIP),一种肠降血糖素,代表胰岛素分泌和葡萄糖稳态的重要调节剂。
编号:114120
CAS号:100040-31-1
单字母:H2N-YAEGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ-OH
| 参考文献(References): | A. Moody et al., FEBS Letters, 123, 205 (1981) |
GIP, human TFA 是一种由 42 个氨基酸组成的肽类激素,是葡萄糖依赖性胰岛素分泌的促进剂和胃酸分泌的弱抑制剂。GIP, human TFA 作为肠 K 细胞释放的肠促胰岛素激素,对营养摄入作出反应。
GIP, human TFA, a peptide hormone consisting of 42 amino acids, is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP, human TFA acts as an incretin hormone released from intestinal K cells in response to nutrient ingestion.
GIP(胃抑制多肽)是一种肽激素,属于肠促胰岛素激素家族。GIP已被证明具有促胰岛素作用,这是通过其激活胰腺β细胞释放葡萄糖依赖性胰岛素来介导的。它还对脂质代谢有影响,并在调节食物摄入方面发挥作用。GIP由回肠和结肠中的K细胞产生,并在进食后释放到血液中。GIP与其受体的结合导致胃酸分泌抑制、胆囊收缩刺激、胃血流量增加、幽门括约肌松弛和胃运动抑制。该产品纯度高(>98%),未检测到内毒素或其他微生物污染。
GIP (Gastric Inhibitory Polypeptide) is a peptide hormone that belongs to the family of incretin hormones. GIP has been shown to have an insulinotropic effect, which is mediated by its activation of glucose-dependent insulin release from pancreatic β-cells. It also has effects on lipid metabolism and plays a role in the regulation of food intake. GIP is produced by K cells in the ileum and colon and released into the bloodstream following food intake. The binding of GIP to its receptors leads to inhibition of gastric acid secretion, stimulation of gallbladder contraction, increased blood flow to the stomach, relaxation of pyloric sphincter muscles, and inhibition of gastric motility. This product is highly pure (> 98%) with no detectable endotoxin or other microbial contamination.
GIP是由小肠细胞产生的肽。GIP已被证明是胰岛素分泌的抑制剂,反过来可能有助于调节葡萄糖水平。它还调节生长激素的释放,以应对食物摄入。GIP充当被称为“胃抑制多肽受体”的受体的配体,该受体存在于胰腺β细胞和十二指肠L细胞上。这种蛋白质已被证明可以激活离子通道并调节其活性。GIP受体也在某些类型的癌症细胞上表达,包括癌症和癌症。已经针对这种蛋白质产生了抗体,用于蛋白质印迹或免疫组织化学等研究工具。
GIP is a peptide that is produced by the cells of the small intestine. GIP has been shown to be an inhibitor of insulin secretion and, in turn, may help regulate glucose levels. It also regulates growth hormone release in response to food intake. GIP acts as a ligand for the receptor known as the “gastric inhibitory polypeptide receptor” which is found on pancreatic beta cells and duodenal L-cells. This protein has been shown to activate ion channels and regulate their activity. The GIP receptor is also expressed on certain types of cancer cells, including breast cancer and colorectal cancer. Antibodies have been generated against this protein for use in research tools such as Western blotting or immunohistochemistry.
分泌是胰岛素分泌和葡萄糖的基本规律。
Incretion is an essential regular of insulin secretion and glucose.
Peptide H-YAEGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ-OH is a Research Peptide with significant interest within the field academic and medical research. Recent citations using H-YAEGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ-OH include the following: Correction: Al-Zamel, N., et al. A Dual GLP-1/GIP Receptor agonist Does Not Antagonize Glucagon at Its Receptor but May Act as a Biased agonist at the GLP-1 N Al-Zamel, S Al-Sabah , Y Luqmani, L Adi - International journal of , 2020 - mdpi.comhttps://www.mdpi.com/1422-0067/21/9/3357 Study on gastric inhibitory polypeptide: Synthesis and properties C Dafu, C Hengran, X Minghua, C Huiting - Acta Biochimica et , 1994 - europepmc.orghttps://europepmc.org/article/cba/272803
| DOI | 名称 | |
|---|---|---|
| 10.1016/s0167-0115(02)00039-3 | Gastric inhibitory polypeptide: the neglected incretin revisited | 下载 |
多肽H2N-Tyr-Ala-Glu-Gly-Thr-Phe-Ile-Ser-Asp-Tyr-Ser-Ile-Ala-Met-Asp-Lys-Ile-His-Gln-Gln-Asp-Phe-Val-Asn-Trp-Leu-Leu-Ala-Gln-Lys-Gly-Lys-Lys-Asn-Asp-Trp-Lys-His-Asn-Ile-Thr-Gln-COOH的合成步骤:
1、合成CTC树脂:称取0.59g CTC Resin(如初始取代度约为0.49mmol/g)和0.35mmol Fmoc-Gln(Trt)-OH于反应器中,加入适量DCM溶解氨基酸(需要注意,此时CTC树脂体积会增大好几倍,避免DCM溶液过少),再加入0.87mmol DIPEA(Mw:129.1,d:0.740g/ml),反应2-3小时后,可不抽滤溶液,直接加入1ml的HPLC级甲醇,封端半小时。依次用DMF洗涤2次,甲醇洗涤1次,DCM洗涤一次,甲醇洗涤一次,DCM洗涤一次,DMF洗涤2次(这里使用甲醇和DCM交替洗涤,是为了更好地去除其他溶质,有利于后续反应)。得到 Fmoc-Gln(Trt)-CTC Resin。结构图如下:

2、脱Fmoc: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-Gln(Trt)-CTC 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0.87mmol Fmoc-Thr(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1.73mmol DIPEA,0.82mmol 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-Thr(tBu)-Gln(Trt)-CTC 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-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Gly-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Gly-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Glu(OtBu)-Gly-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Glu(OtBu)-Gly-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Ala-Glu(OtBu)-Gly-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
H2N-Ala-Glu(OtBu)-Gly-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC Resin
Fmoc-Tyr(tBu)-Ala-Glu(OtBu)-Gly-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC 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)-Ala-Glu(OtBu)-Gly-Thr(tBu)-Phe-Ile-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-Ile-Ala-Met-Asp(OtBu)-Lys(Boc)-Ile-His(Trt)-Gln(Trt)-Gln(Trt)-Asp(OtBu)-Phe-Val-Asn(Trt)-Trp(Boc)-Leu-Leu-Ala-Gln(Trt)-Lys(Boc)-Gly-Lys(Boc)-Lys(Boc)-Asn(Trt)-Asp(OtBu)-Trp(Boc)-Lys(Boc)-His(Trt)-Asn(Trt)-Ile-Thr(tBu)-Gln(Trt)-CTC 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-Ala-Glu-Gly-Thr-Phe-Ile-Ser-Asp-Tyr-Ser-Ile-Ala-Met-Asp-Lys-Ile-His-Gln-Gln-Asp-Phe-Val-Asn-Trp-Leu-Leu-Ala-Gln-Lys-Gly-Lys-Lys-Asn-Asp-Trp-Lys-His-Asn-Ile-Thr-Gln-COOH。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。





