专肽生物_定制多肽合成服务_多肽合成定制服务_多肽合成厂家_多肽合成公司

Super-TDU 是一种特异性的 YAP 拮抗剂，可以靶向 YAP-TEAD 相互作用。Super-TDU 可以抑制胃癌小鼠模型的肿瘤生长。
Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model[1].

Super-TDU 是一种特异性的YAP拮抗剂，可以靶向YAP-TEAD相互作用。Super-TDU可以抑制胃癌小鼠模型的肿瘤生长。 Ser-Val-Asp-Asp-His-Phe-Ala-Lys-Ser-Leu-Gly-Asp-Thr-Trp-Leu-Gln-Ile-Gly-Gly-Ser-Gly-Asn-Pro-Lys-Thr-Ala-Asn-Val-Pro-Gln-Thr-Val-Pro-Met-Arg-Leu-Arg-Lys-Leu-Pro-Asp-Ser-Phe-Phe-Lys-Pro-Pro-Glu 体外研究： Super-TDU 下调 YAP-TEADs 靶基因 CTGF、CYR61 和 CDX2 的表达。Super-TDU 抑制 GC 细胞系 MGC -803、BGC-823 和 HGC27 的细胞活力和集落形成。 体内研究： Super-TDU (静脉注射；50 μg/kg 或 500 μg/kg；每天) 显著降低小鼠肿瘤的大小、重量和 YAP 靶基因，呈剂量依赖性。 Super-TDU (静脉注射；250 μg/kg 500 μg/kg) t1/2α 分别为 0.78 小时和 0.82 小时；6.12 ng/mL 和 13.3 ng/mL 的 Cmax；250 μg/kg 和 500 μg/kg 小鼠的 CL 分别为 7.41 mL/min/kg 和 7.72 mL/min/kg。
 

多肽H2N-Ser-Val-Asp-Asp-His-Phe-Ala-Lys-Ser-Leu-Gly-Asp-Thr-Trp-Leu-Gln-Ile-Gly-Gly-Ser-Gly-Asn-Pro-Lys-Thr-Ala-Asn-Val-Pro-Gln-Thr-Val-Pro-Met-Arg-Leu-Arg-Lys-Leu-Pro-Asp-Ser-Phe-Phe-Lys-Pro-Pro-Glu-COOH的合成步骤：

1、合成CTC树脂：称取2.67g CTC Resin（如初始取代度约为0.61mmol/g）和1.95mmol Fmoc-Glu(OtBu)-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4.89mmol 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-Glu(OtBu)-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-Glu(OtBu)-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4.89mmol Fmoc-Pro-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9.77mmol DIPEA，4.64mmol 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-Pro-Glu(OtBu)-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-Pro-Glu(OtBu)-CTC Resin

Fmoc-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Asp(OtBu)-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Asp(OtBu)-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Asp(OtBu)-Asp(OtBu)-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Asp(OtBu)-Asp(OtBu)-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Val-Asp(OtBu)-Asp(OtBu)-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

H2N-Val-Asp(OtBu)-Asp(OtBu)-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-CTC Resin

Fmoc-Ser(tBu)-Val-Asp(OtBu)-Asp(OtBu)-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-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-Ser(tBu)-Val-Asp(OtBu)-Asp(OtBu)-His(Trt)-Phe-Ala-Lys(Boc)-Ser(tBu)-Leu-Gly-Asp(OtBu)-Thr(tBu)-Trp(Boc)-Leu-Gln(Trt)-Ile-Gly-Gly-Ser(tBu)-Gly-Asn(Trt)-Pro-Lys(Boc)-Thr(tBu)-Ala-Asn(Trt)-Val-Pro-Gln(Trt)-Thr(tBu)-Val-Pro-Met-Arg(Pbf)-Leu-Arg(Pbf)-Lys(Boc)-Leu-Pro-Asp(OtBu)-Ser(tBu)-Phe-Phe-Lys(Boc)-Pro-Pro-Glu(OtBu)-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-Ser-Val-Asp-Asp-His-Phe-Ala-Lys-Ser-Leu-Gly-Asp-Thr-Trp-Leu-Gln-Ile-Gly-Gly-Ser-Gly-Asn-Pro-Lys-Thr-Ala-Asn-Val-Pro-Gln-Thr-Val-Pro-Met-Arg-Leu-Arg-Lys-Leu-Pro-Asp-Ser-Phe-Phe-Lys-Pro-Pro-Glu-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。