400-998-5282
专注多肽 服务科研
400-998-5282
专注多肽 服务科研
PACAP（1-27），人、绵羊、大鼠醋酸盐是一种最初从牛下丘脑中分离的神经肽，也存在于人和大鼠中。它是一种强效的PACAP受体激动剂。
编号：129060
CAS号：127317-03-7
单字母：H2N-HSDGIFTDSYSRYRKQMAVKKYLAAVL-CONH2
| 参考文献（References）: | A. Miyata et al., BBRC, 164, 567 (1989) A. Mirata et al., Regulatory Peptides, 26, 170 (1989) |
PACAP (1-27), human, ovine, rat (PACAP 1-27) 是 PACAP-38 的 N-末端片段，是一种有效的 PACAP 受体拮抗剂，对大鼠 PAC1，大鼠 VPAC1 和人 VPAC2 的 IC50 值分别为 3 nM，2 nM 和 5 nM。
PACAP (1-27), human, ovine, rat (PACAP 1-27) is the N-terminal fragment of PACAP-38, and is a potent PACAP receptor antagonist with IC50s of 3 nM, 2 nM and 5 nM for rat PAC1, rat VPAC1 and human VPAC2, respectively.
PACAP（1-27），人、绵羊、大鼠醋酸盐是一种最初从牛下丘脑中分离的神经肽，也存在于人和大鼠中。它是一种强效的PACAP受体激动剂。
PACAP (1-27), human, ovine, rat acetate is a neuropeptide originally isolated from the bovine hypothalamus, also found in humans and rats. It is a potent PACAP receptor agonist.
PACAP27是一种用作研究工具的肽。PACAP27与垂体腺苷酸环化酶激活多肽（PACAP）的受体结合。PACAP27与受体的结合导致腺苷酸环化酶的激活，从而增加细胞内cAMP的水平。cAMP的这种增加可能导致细胞反应，例如离子通道活性增加和蛋白质合成增加。
PACAP27 is a peptide that is used as a research tool. PACAP27 binds to the receptor for pituitary adenylate cyclase-activating polypeptide (PACAP). The binding of PACAP27 to the receptor leads to activation of adenylyl cyclase, which increases intracellular levels of cAMP. This increase in cAMP may lead to cellular responses such as increased ion channel activity and increased protein synthesis.
PACAP 1-27（垂体腺苷酸环化酶激活多肽27）是腺苷酸环化酶的有效刺激剂，可增加cAMP水平。
PACAP 1-27 (Pituitary adenylate cyclase-activating polypeptide 27) is a potent stimulator of adenylyl cyclase and increases cAMP levels.
PACAP-38及其N端片段PACAP-27是最初从牛下丘脑分离的新型神经肽。它们也存在于人类和老鼠身上。PACAP-27和PACAP-38与血管活性肠多肽（VIP）具有相当大的同源性，可以比VIP更有效地刺激腺苷酸环化酶。
PACAP-38 and its N-terminal fragment PACAP-27 are novel neuropeptides originally isolated from bovine hypothalamus. They are also found in humans and rats. Both PACAP-27 and PACAP-38, showing considerable homology with vasoactive intestinal polypeptide (VIP), can stimulate adenylate cyclase much more potently than VIP.
PACAP-27（人、小鼠、羊、猪、大鼠）具有 PACAP 序列的缩短形式，具有强螺旋形成行为。保守残基支持跨物种受体结合分析。折叠转变允许功能基序的探索。其应用涵盖神经肽生物合成、合成设计和结构生物学研究。
PACAP-27 (human, mouse, ovine, porcine, rat) features a shortened form of the PACAP sequence with strong helicogenic behavior. Conserved residues support cross-species receptor-binding analysis. Folding transitions allow exploration of functional motifs. Its applications span neuropeptide biosynthesis, synthetic design, and structural biology research.
| DOI | 名称 | |
|---|---|---|
| 10.1016/s0167-0115(98)00147-5 | Structural motifs of pituitary adenylate cyclase-activating polypeptide (PACAP) defining PAC1-receptor selectivity | 下载 |
| 10.1111/j.1476-5381.1995.tb15897.x | Inhibition of bronchoconstriction by pituitary adenylate cyclase activating polypeptide (PACAP 1-27) in guinea-pigs in vivo | 下载 |
| 10.1016/0014-2999(95)00467-5 | Fragments of pituitary adenylate cyclase activating polypeptide discriminate between type I and II recombinant receptors | 下载 |
多肽H2N-His-Ser-Asp-Gly-Ile-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Ala-Ala-Val-Leu-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2.51g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2.26mmol Fmoc-Leu-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4.52mmol DIPEA，2.15mmol 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-Leu-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-Leu-Linker-MBHA Resin
Fmoc-Val-Leu-Linker-MBHA Resin
H2N-Val-Leu-Linker-MBHA Resin
Fmoc-Ala-Val-Leu-Linker-MBHA Resin
H2N-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Gly-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Gly-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Asp(OtBu)-Gly-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Asp(OtBu)-Gly-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-Ser(tBu)-Asp(OtBu)-Gly-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
H2N-Ser(tBu)-Asp(OtBu)-Gly-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-Linker-MBHA Resin
Fmoc-His(Trt)-Ser(tBu)-Asp(OtBu)-Gly-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-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-His(Trt)-Ser(tBu)-Asp(OtBu)-Gly-Ile-Phe-Thr(tBu)-Asp(OtBu)-Ser(tBu)-Tyr(tBu)-Ser(tBu)-Arg(Pbf)-Tyr(tBu)-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Ala-Ala-Val-Leu-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-His-Ser-Asp-Gly-Ile-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Ala-Ala-Val-Leu-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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