133514-43-9_Exendin(9-39)_H2N-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-CONH2_H2N-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-CONH2_未分类肽

多肽产品

Exendin(9-39)
Exendin（9-39）是一种有效的胰高血糖素样肽1（GLP-1）受体拮抗剂。它也被描述为推定的exendin受体的拮抗剂。Exendin（9-39）阻断GLP-1（7-36）酰胺和Exendin-4对胰腺腺泡cAMP产生的刺激作用。

编号：110858

CAS号：133514-43-9

单字母：H2N-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-CONH2

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编号:	110858
中文名称:	Exendin(9-39)
英文名:	Exendin(9-39)
CAS号:	133514-43-9
单字母:	H2N-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-CONH2
三字母:	H2N N端氨基：N-terminal amino group。在肽或多肽链中含有游离a-氨基的氨基酸一端。在表示氨基酸序列时，通常将N端放在肽链的左边。 -Asp L-天冬氨酸：aspartic acid。系统命名为(2S)-氨基-丁二酸。是编码氨基酸，又是神经递质。符号：D，Asp。D-天冬氨酸存在于多种细菌的细胞壁和短杆菌肽A中。 -Leu L-亮氨酸：leucine。系统命名为(2S)-氨基-4-甲基戊酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号：L，Leu。 -Ser L-丝氨酸：serine。系统命名为(2S)-氨基-3-羟基丙酸。是编码氨基酸。因可从蚕丝中获得而得名。符号：S，Ser。在丝原蛋白及某些抗菌素中含有 D-丝氨酸。 -Lys L-赖氨酸：lysine。系统命名为(2S)-6-二氨基已酸。是编码氨基酸中的碱性氨基酸，哺乳动物的必需氨基酸。在蛋白质中的赖氨酸可以被修饰为多种形式的衍生物。符号：K，Lys。 -Gln L-谷氨酰胺：glutamine。系统命名为(2S)-氨基-4-氨酰基丁酸，是编码氨基酸。符号：GIn，Q。 -Met L-甲硫氨酸：methionine又称“蛋氨酸”。系统命名为(2S)-氨基-4-甲硫基丁酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号：M，Met。 -Glu L-谷氨酸：glutamic acid。系统命名为(2S)-氨基-戊二酸。是编码氨基酸。符号：E，Glu。D-谷氨酸存在于多种细菌的细胞壁和某些细菌杆菌肽中。 -Glu L-谷氨酸：glutamic acid。系统命名为(2S)-氨基-戊二酸。是编码氨基酸。符号：E，Glu。D-谷氨酸存在于多种细菌的细胞壁和某些细菌杆菌肽中。 -Glu L-谷氨酸：glutamic acid。系统命名为(2S)-氨基-戊二酸。是编码氨基酸。符号：E，Glu。D-谷氨酸存在于多种细菌的细胞壁和某些细菌杆菌肽中。 -Ala 丙氨酸：alanine。L-丙氨酸的系统命名为(2S)-氨基丙酸，是编码氨基酸，也叫L-α-丙氨酸。符号：A，Ala。D-丙氨酸存在于多种细菌细胞壁的糖肽中。β-丙氨酸是维生素泛酸和辅酶A的组分。 -Val L-缬氨酸：valine。系统命名为(2S)-氨基-3-甲基丁酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号：V，Val。在某些放线菌素如缬霉素中存在 D-缬氨酸。 -Arg L-精氨酸：arginine。系统命名为(2S)-氨基-5-胍基戊酸。在生理条件下带正电荷，为编码氨基酸。是幼小哺乳动物的必需氨基酸。符号：R，Arg。 -Leu L-亮氨酸：leucine。系统命名为(2S)-氨基-4-甲基戊酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号：L，Leu。 -Phe L-苯丙氨酸：phenylalanine。系统命名为(2S)-氨基-3-苯基丙酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号：F，Phe。 -Ile L-异亮氨酸：isoleucine。系统命名为(2S)-氨基-(3R)-甲基戊酸。是编码氨基酸。有两个手性碳原子，是哺乳动物的必需氨基酸。符号:I，Ile。 -Glu L-谷氨酸：glutamic acid。系统命名为(2S)-氨基-戊二酸。是编码氨基酸。符号：E，Glu。D-谷氨酸存在于多种细菌的细胞壁和某些细菌杆菌肽中。 -Trp L-色氨酸：tryptophan[e]。系统命名为(2S)-氨基-3-(3-吲哚基)丙酸。是编码氨基酸，哺乳动物的必需氨基酸。符号：W，Trp。某些抗菌素中含有 D-色氨酸。 -Leu L-亮氨酸：leucine。系统命名为(2S)-氨基-4-甲基戊酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号：L，Leu。 -Lys L-赖氨酸：lysine。系统命名为(2S)-6-二氨基已酸。是编码氨基酸中的碱性氨基酸，哺乳动物的必需氨基酸。在蛋白质中的赖氨酸可以被修饰为多种形式的衍生物。符号：K，Lys。 -Asn 天冬酰胺：asparagine。L-天冬酰胺的系统命名为(2S)-氨基-3-氨酰基丙酸，是编码氨基酸。符号：N，Asn。D-天冬酰胺存在于短杆菌肽A分子中。 -Gly 甘氨酸：glycine。系统命名为 2-氨基乙酸。是编码氨基酸中没有旋光性的最简单的氨基酸，因具有甜味而得名。符号：G，Gly。 -Gly 甘氨酸：glycine。系统命名为 2-氨基乙酸。是编码氨基酸中没有旋光性的最简单的氨基酸，因具有甜味而得名。符号：G，Gly。 -Pro L-脯氨酸：proline。系统命名为吡咯烷-(2S)-羧酸。为亚氨基酸。是编码氨基酸。在肽链中有特殊作用，如易形成顺式的肽键等。符号：P，Pro。 -Ser L-丝氨酸：serine。系统命名为(2S)-氨基-3-羟基丙酸。是编码氨基酸。因可从蚕丝中获得而得名。符号：S，Ser。在丝原蛋白及某些抗菌素中含有 D-丝氨酸。 -Ser L-丝氨酸：serine。系统命名为(2S)-氨基-3-羟基丙酸。是编码氨基酸。因可从蚕丝中获得而得名。符号：S，Ser。在丝原蛋白及某些抗菌素中含有 D-丝氨酸。 -Gly 甘氨酸：glycine。系统命名为 2-氨基乙酸。是编码氨基酸中没有旋光性的最简单的氨基酸，因具有甜味而得名。符号：G，Gly。 -Ala 丙氨酸：alanine。L-丙氨酸的系统命名为(2S)-氨基丙酸，是编码氨基酸，也叫L-α-丙氨酸。符号：A，Ala。D-丙氨酸存在于多种细菌细胞壁的糖肽中。β-丙氨酸是维生素泛酸和辅酶A的组分。 -Pro L-脯氨酸：proline。系统命名为吡咯烷-(2S)-羧酸。为亚氨基酸。是编码氨基酸。在肽链中有特殊作用，如易形成顺式的肽键等。符号：P，Pro。 -Pro L-脯氨酸：proline。系统命名为吡咯烷-(2S)-羧酸。为亚氨基酸。是编码氨基酸。在肽链中有特殊作用，如易形成顺式的肽键等。符号：P，Pro。 -Pro L-脯氨酸：proline。系统命名为吡咯烷-(2S)-羧酸。为亚氨基酸。是编码氨基酸。在肽链中有特殊作用，如易形成顺式的肽键等。符号：P，Pro。 -Ser L-丝氨酸：serine。系统命名为(2S)-氨基-3-羟基丙酸。是编码氨基酸。因可从蚕丝中获得而得名。符号：S，Ser。在丝原蛋白及某些抗菌素中含有 D-丝氨酸。 -CONH2 C端酰胺化
氨基酸个数:	31
分子式:	C₁₄₉H₂₃₄N₄₀O₄₇S₁
平均分子量:	3369.76
精确分子量:	3367.69
等电点(PI):	4.67
pH=7.0时的净电荷数:	-1.02
酸性基团个数:	-0.99
碱性基团个数:	亲水
平均亲水性:	0.3625
疏水性值:	-0.65
外观与性状:	白色粉末状固体
消光系数:	5500
来源:	人工化学合成，仅限科学研究使用，不得用于人体。
纯度:	95%、98%
盐体系:	可选TFA、HAc、HCl或其它
储存条件:	负80℃至负20℃
标签:	未分类肽

参考文献（References）:

Greig, NH. et al. Diabetolog 42, 45 (1999) Montrose-Rafizadeh, C. et al. J Biol Chem 272, 21201 (1997) Göke R. et al. J Biol Chem 268, 19650 (1993) Eng, J. et al. J Biol Chem 267, 7402 (1992)

Exendin（9-39）是一种有效的胰高血糖素样肽1（GLP-1）受体拮抗剂。它也被描述为推定的exendin受体的拮抗剂。Exendin（9-39）阻断GLP-1（7-36）酰胺和Exendin-4对胰腺腺泡cAMP产生的刺激作用。此外，exendin（9-39）被证明可安全地用于消除GLP-1的肠促胰岛素效应，而不干扰循环营养素对胰岛素分泌的控制。

Exendin (9-39) is a potent glucagon-like peptide 1 (GLP-1) receptor antagonist. It has also been described as an antagonist of the putative exendin receptor. Exendin (9-39) blocks the stimulatory action of GLP-1 (7- 36) amide and of exendin-4 on cAMP production in pancreatic acini. Moreover, exendin (9-39) was shown to be safely used to abolish the incretin effect of GLP-1 without interfering with the control of insulin secretion by circulating nutrients.

Exendin（9-39）对胰高血糖素样肽1（GLP-1）具有选择性和强效性，并抑制由胃抑制肽（GIP）引起的cAMP产生（Kd=1.7nm）。Exendin（9-39）通过减少胰岛素分泌参与食欲调节，有助于防止血糖水平急剧下降。这种肽已经被研究过了吗？对基底微血管通透性的影响。

Exendin (9-39) is a selective and potent against glucagon-like peptide 1 (GLP-1) and inhibits (Kd = 1.7 nm) cAMP production caused by Gastric Inhibitory Peptide (GIP). Exendin (9-39) is involved in appetite modulation by reducing insulin secretion and helps prevent sharp falls in glucose levels. This peptide has been studied for its? effects on the permeability of basal microvascular.

Exendin(9-39) amide (Avexitide) 是一种胰高血糖素样肽-1 (GLP-1) 拮抗剂，能够与内源性 GLP-1 竞争结合 GLP-1 受体，从而对抗过量 GLP-1 分泌的影响。Exendin(9-39) amide 可用于研究术后低血糖症 (PBH)。

对于对药物治疗无反应的KATP通道突变型（KATPHI）患者，需通过胰腺切除术控制低血糖。临床前研究显示，GLP-1受体拮抗剂艾塞那肽-（9-39）可抑制胰岛素分泌，并改善SUR-12/2小鼠的空腹低血糖症状。

Exendin (9-39) Amide 是一种长效胰高血糖素样肽 1（GLP-1）受体拮抗剂。GLP-1 是一种肠促胰岛素激素，正常情况下，GLP-1 与胰岛 β 细胞表面的 GLP-1 受体结合，通过 G 蛋白偶联机制，激活腺苷酸环化酶，使细胞内 cAMP 水平升高，进一步激活蛋白激酶 A，从而促进胰岛素的分泌。Exendin (9-39) Amide 能竞争性地与 GLP-1 受体结合，阻断 GLP-1 与受体的正常结合，进而抑制胰岛素的分泌。此外，在中枢神经系统中，GLP-1 参与调控食欲和能量平衡，Exendin (9-39) Amide 通过阻断 GLP-1 信号通路，影响机体对食欲的调节机制，改变能量摄入和代谢。

参考文献

Calabria AC, et al. GLP-1 receptor antagonist exendin-(9-39) elevates fasting blood glucose levels in congenital owing to inactivating mutations in the ATP-sensitive K+ channel. Diabetes. 2012 Oct;61(10):2585-91

Exendin(9-39) amide 同义词：Avexitide Avexitide (Exendin (9-39)) 是特异竞争性的 glucagon-like peptide-1 (GLP-1) 受体拮抗剂。体外研究： GLP-1 plays a role in the control of fasting glucose. Avexitide (Exendin (9-39)), a truncated form of the GLP-1 agonist exendin-4, is a specific GLP-1 receptor antagonist。体内研究： Continuous subcutaneous infusion of Avexitide (Exendin (9-39)) significantly raises fasting blood glucose levels in SUR-1 -/- mice without affecting glucose tolerance。 H2O 中的溶解度 : 50 mg/mL (14.84 mM; 超声助溶)

DOI	名称
10.1055/s-2002-19960	Resistance of succinic acid dimethyl ester insulinotropic action to exendin (9-39) amide	下载
10.1038/sj.bjp.0705453	A model for receptor-peptide binding at the glucagon-like peptide-1 (GLP-1) receptor through the analysis of truncated ligands and receptors	下载
10.1016/s0014-5793(03)01043-3	The positive charge at Lys-288 of the glucagon-like peptide-1 (GLP-1) receptor is important for binding the N-terminus of peptide agonists	下载
10.1172/JCI25764	Brain glucagon-like peptide-1 increases insulin secretion and muscle insulin resistance to favor hepatic glycogen storage	下载
10.1016/j.regpep.2007.10.001	Protective effects of GLP-1 analogues exendin-4 and GLP-1(9-36) amide against ischemia-reperfusion injury in rat heart	下载
10.1007/s11605-009-0912-9	Duodenal-jejunal exclusion improves glucose tolerance in the diabetic, Goto-Kakizaki rat by a GLP-1 receptor-mediated mechanism	下载
10.1113/jphysiol.2009.175067	Vagally mediated effects of glucagon-like peptide 1: in vitro and in vivo gastric actions	下载
10.1152/ajprenal.00082.2009	Regulation of Na+/H+ exchanger NHE3 by glucagon-like peptide 1 receptor agonist exendin-4 in renal proximal tubule cells	下载
10.1007/s00125-009-1611-5	The glucagon-like peptide 1 receptor is essential for postprandial lipoprotein synthesis and secretion in hamsters and mice	下载
10.1124/jpet.110.166009	Comparative effects of the endogenous agonist glucagon-like peptide-1 (GLP-1)-(7-36) amide and the small-molecule ago-allosteric agent "compound 2" at the GLP-1 receptor	下载
10.1186/1475-2840-10-6	Glucagon-like peptide-1 enhances cardiac L-type Ca2+ currents via activation of the cAMP-dependent protein kinase A pathway	下载
10.1007/s00125-010-2028-x	Glucagon-like peptide-1 receptor agonist ameliorates renal injury through its anti-inflammatory action without lowering blood glucose level in a rat model of type 1 diabetes	下载
10.1186/1471-230X-12-30	Glucagon-like peptides 1 and 2 and vasoactive intestinal peptide are neuroprotective on cultured and mast cell co-cultured rat myenteric neurons	下载
10.1172/JCI57256	An anti-diabetes agent protects the mouse brain from defective insulin signaling caused by Alzheimer's disease- associated Aβ oligomers	下载
10.1016/j.regpep.2012.06.007	Postconditioning with curaglutide, a novel GLP-1 analog, protects against heart ischemia-reperfusion injury in an isolated rat heart	下载
10.1016/j.regpep.2012.08.009	Receptor-mediated inhibition of small bowel migrating complex by GLP-1 analog ROSE-010 delivered via pulmonary and systemic routes in the conscious rat	下载
10.1038/jcbfm.2012.133	Liraglutide, a long-acting GLP-1 mimetic, and its metabolite attenuate inflammation after intracerebral hemorrhage	下载
10.1210/jc.2013-1029	The DPP-4 inhibitor linagliptin restores β-cell function and survival in human isolated islets through GLP-1 stabilization	下载
10.1007/s00595-013-0638-x	Effects of duodeno-jejunal bypass on glucose metabolism in obese rats with type 2 diabetes	下载
10.1172/JCI68459	Lipotoxicity disrupts incretin-regulated human β cell connectivity	下载
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10.1016/0196-9781(94)90204-6	Stable expression of the rat GLP-I receptor in CHO cells: activation and binding characteristics utilizing GLP-I(7-36)-amide, oxyntomodulin, exendin-4, and exendin(9-39)	下载
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多肽H2N-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-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2.17g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1.95mmol Fmoc-Ser(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3.91mmol DIPEA，1.86mmol 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-Ser(tBu)-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-Ser(tBu)-Linker-MBHA Resin

Fmoc-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Ala-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Ala-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Glu(OtBu)-Ala-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Glu(OtBu)-Ala-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Glu(OtBu)-Glu(OtBu)-Ala-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Glu(OtBu)-Glu(OtBu)-Ala-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

Fmoc-Glu(OtBu)-Glu(OtBu)-Glu(OtBu)-Ala-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

H2N-Glu(OtBu)-Glu(OtBu)-Glu(OtBu)-Ala-Val-Arg(Pbf)-Leu-Phe-Ile-Glu(OtBu)-Trp(Boc)-Leu-Lys(Boc)-Asn(Trt)-Gly-Gly-Pro-Ser(tBu)-Ser(tBu)-Gly-Ala-Pro-Pro-Pro-Ser(tBu)-Linker-MBHA Resin

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

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

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

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

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

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

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

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

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

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

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

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。
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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

多肽产品

Exendin(9-39)
Exendin（9-39）是一种有效的胰高血糖素样肽1（GLP-1）受体拮抗剂。它也被描述为推定的exendin受体的拮抗剂。Exendin（9-39）阻断GLP-1（7-36）酰胺和Exendin-4对胰腺腺泡cAMP产生的刺激作用。

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多肽产品

Exendin(9-39)Exendin（9-39）是一种有效的胰高血糖素样肽1（GLP-1）受体拮抗剂。它也被描述为推定的exendin受体的拮抗剂。Exendin（9-39）阻断GLP-1（7-36）酰胺和Exendin-4对胰腺腺泡cAMP产生的刺激作用。

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打开微信扫一扫

在线留言

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Exendin(9-39)
Exendin（9-39）是一种有效的胰高血糖素样肽1（GLP-1）受体拮抗剂。它也被描述为推定的exendin受体的拮抗剂。Exendin（9-39）阻断GLP-1（7-36）酰胺和Exendin-4对胰腺腺泡cAMP产生的刺激作用。