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專注多肽 服務(wù)科研
PG 99-465 是一種高親和力、選擇性的 VPAC2 受體拮抗劑。該化合物對 VPAC1 受體顯示出部分激動活性。
編號：200403
CAS號：2243219-86-3
單字母：Myristicacid-HSDAVFTDNYTKLRKQMAVKKYLNSIKKGGT-OH
| 編號: | 200403 |
| 中文名稱: | 血管活性腸肽Myristoyl-(Lys12.27.28)-VIP-Gly-Gly-Thr (free acid) |
| 英文名: | Myristoyl-(Lys12.27.28)-VIP-Gly-Gly-Thr (free acid) |
| CAS號: | 2243219-86-3 |
| 單字母: | Myristicacid-HSDAVFTDNYTKLRKQMAVKKYLNSIKKGGT-OH |
| 三字母: | Myristicacid N端肉豆蔻酸修飾 -His組氨酸 -Ser絲氨酸 -Asp天冬氨酸 -Ala丙氨酸 -Val纈氨酸 -Phe苯丙氨酸 -Thr蘇氨酸 -Asp天冬氨酸 -Asn天冬酰胺 -Tyr酪氨酸 -Thr蘇氨酸 -Lys賴氨酸 -Leu亮氨酸 -Arg精氨酸 -Lys賴氨酸 -Gln谷氨酰胺 -Met甲硫氨酸 -Ala丙氨酸 -Val纈氨酸 -Lys賴氨酸 -Lys賴氨酸 -Tyr酪氨酸 -Leu亮氨酸 -Asn天冬酰胺 -Ser絲氨酸 -Ile異亮氨酸 -Lys賴氨酸 -Lys賴氨酸 -Gly甘氨酸 -Gly甘氨酸 -Thr蘇氨酸 -OHC端羧基 |
| 氨基酸個數(shù): | 31 |
| 分子式: | C171H283O47N45S1 |
| 平均分子量: | 3753.42 |
| 精確分子量: | 3751.09 |
| 等電點(PI): | 11.5 |
| pH=7.0時的凈電荷數(shù): | 7.24 |
| 平均親水性: | 0.22413793103448 |
| 疏水性值: | -0.84 |
| 消光系數(shù): | 2980 |
| 來源: | 人工化學(xué)合成，僅限科學(xué)研究使用，不得用于人體。 |
| 儲存條件: | 負(fù)80℃至負(fù)20℃ |
| 標(biāo)簽: | 烷基化肽 |
PG 99-465 is a high affinity, selective VPAC2 receptor antagonist. It exhibited a 100-fold preference for the VPAC2 over the VPAC1 receptor. The compound showed partial agonistic activity on the VPAC1 receptor and was inactive on the VPAC2 receptor transfected in CHO cells, as well as on naturally expressed human VPAC2 receptors in the SUP T1 cell line. Dickson et al. observed an agonistic effect of PG99-465 on the human VPAC1 and PAC1 receptors. When applied singly, PG99-465 increased [cAMP](i) at all three hVPAC/PAC receptor subtypes.
烷基化肽-說明
專肽生物可提供多肽烷基化修飾，增加多肽一端的疏水性，例如常見的C18，C16，C14，C12，以及C6等，也可根據(jù)客戶要求，接其他長度的烷基化鏈。
| DOI | 名稱 | |
|---|---|---|
| 10.1046/j.1365-2826.2002.00826.x | Effects of vasoactive intestinal polypeptide on neurones of the rat suprachiasmatic nuclei in vitro | 下載 |
| 10.1046/j.1460-9568.2003.02425.x | The mouse VPAC2 receptor confers suprachiasmatic nuclei cellular rhythmicity and responsiveness to vasoactive intestinal polypeptide in vitro | 下載 |
| 10.1038/sj.bjp.0705918 | Inhibitory pathways in the circular muscle of rat jejunum | 下載 |
| 10.1016/j.brainres.2005.04.077 | VIP enhances synaptic transmission to hippocampal CA1 pyramidal cells through activation of both VPAC1 and VPAC2 receptors | 下載 |
| 10.1016/j.neuropharm.2006.07.017 | A systematic comparison of intracellular cyclic AMP and calcium signalling highlights complexities in human VPAC/PAC receptor pharmacology | 下載 |
| 10.1124/mol.109.060137 | Identification and characterization of a small molecule antagonist of human VPAC(2) receptor | 下載 |
| 10.1016/j.neuron.2013.06.026 | Translational control of entrainment and synchrony of the suprachiasmatic circadian clock by mTOR/4E-BP1 signaling | 下載 |
| 10.1002/syn.21772 | Augmented cystine-glutamate exchange by pituitary adenylate cyclase-activating polypeptide signaling via the VPAC1 receptor | 下載 |
| 10.1002/jez.1964 | Sex steroid hormone secretion in the wall lizard Podarcis sicula testis: The involvement of VIP | 下載 |
多肽Myristicacid-His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Lys-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Lys-Lys-Gly-Gly-Thr-COOH的合成步驟：
1、合成CTC樹脂：稱取2.16g CTC Resin（如初始取代度約為1.04mmol/g）和2.7mmol Fmoc-Thr(tBu)-OH于反應(yīng)器中，加入適量DCM溶解氨基酸（需要注意，此時CTC樹脂體積會增大好幾倍，避免DCM溶液過少），再加入6.74mmol DIPEA（Mw：129.1,d：0.740g/ml），反應(yīng)2-3小時后，可不抽濾溶液，直接加入1ml的HPLC級甲醇，封端半小時。依次用DMF洗滌2次，甲醇洗滌1次，DCM洗滌一次，甲醇洗滌一次，DCM洗滌一次，DMF洗滌2次（這里使用甲醇和DCM交替洗滌，是為了更好地去除其他溶質(zhì)，有利于后續(xù)反應(yīng)）。得到 Fmoc-Thr(tBu)-CTC Resin。結(jié)構(gòu)圖如下：
2、脫Fmoc：加3倍樹脂體積的20%Pip/DMF溶液，鼓氮氣30分鐘，然后2倍樹脂體積的DMF 洗滌5次。得到 H2N-Thr(tBu)-CTC Resin 。（此步驟脫除Fmoc基團，茚三酮檢測為藍(lán)色，Pip為哌啶）。結(jié)構(gòu)圖如下：
3、縮合：取6.74mmol Fmoc-Gly-OH 氨基酸，加入到上述樹脂里，加適當(dāng)DMF溶解氨基酸，再依次加入13.48mmol DIPEA，6.4mmol HBTU。反應(yīng)30分鐘后，取小樣洗滌，茚三酮檢測為無色。用2倍樹脂體積的DMF 洗滌3次樹脂。（洗滌樹脂，去掉殘留溶劑，為下一步反應(yīng)做準(zhǔn)備）。得到Fmoc-Gly-Thr(tBu)-CTC Resin。氨基酸：DIPEA：HBTU：樹脂=3：6：2.85：1（摩爾比）。結(jié)構(gòu)圖如下：
4、依次循環(huán)步驟二、步驟三，依次得到
H2N-Gly-Thr(tBu)-CTC Resin
Fmoc-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-His(Trt)-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
以上中間結(jié)構(gòu)，均可在專肽生物多肽計算器-多肽結(jié)構(gòu)計算器中，一鍵畫出。
最后再經(jīng)過步驟二得到 H2N-His(Trt)-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin，結(jié)構(gòu)如下：
5、肉豆蔻酸反應(yīng)連接：在上述樹脂中，加入適當(dāng)DMF后，再加入6.74mmol 肉豆蔻酸到樹脂中，再加入13.48mmol DIPEA、6.4mmol HBTU，鼓氮氣反應(yīng)30分鐘。用2倍樹脂體積的DMF 洗滌3次樹脂（洗滌樹脂，去掉殘留溶劑，為下一步反應(yīng)做準(zhǔn)備）。 得到Myristicacid-His(Trt)-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTCResin。 結(jié)構(gòu)如下：
6、切割：6倍樹脂體積的切割液（或每1g樹脂加8ml左右的切割液），搖床搖晃 2小時，過濾掉樹脂，用冰無水乙醚沉淀濾液，并用冰無水乙醚洗滌沉淀物3次，最后將沉淀物放真空干燥釜中，常溫干燥24小試，得到粗品Myristicacid-His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Lys-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Lys-Lys-Gly-Gly-Thr-COOH。結(jié)構(gòu)圖見產(chǎn)品結(jié)構(gòu)圖。
切割液選擇：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%
（前兩種適合沒有容易氧化的氨基酸，例如Trp、Cys、Met。第三種適合幾乎所有的序列。）
6、純化凍干：使用液相色譜純化，收集目標(biāo)峰液體，進行凍干，獲得蓬松的粉末狀固體多肽。不過這時要取小樣復(fù)測下純度 是否目標(biāo)純度。
7、最后總結(jié)：
杭州專肽生物技術(shù)有限公司（ALLPEPTIDE http://amynixphotography.com）主營定制多肽合成業(yè)務(wù)，提供各類長肽，短肽，環(huán)肽，提供各類修飾肽，如：熒光標(biāo)記修飾（CY3、CY5、CY5.5、CY7、FAM、FITC、Rhodamine B、TAMRA等），功能基團修飾肽（疊氮、炔基、DBCO、DOTA、NOTA等），同位素標(biāo)記肽（N15、C13），訂書肽（Stapled Peptide）,脂肪酸修飾肽（Pal、Myr、Ste），磷酸化修飾肽（P-Ser、P-Thr、P-Tyr），環(huán)肽（酰胺鍵環(huán)肽、一對或者多對二硫鍵環(huán)），生物素標(biāo)記肽，PEG修飾肽，甲基化修飾肽等。
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