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抑制剂/激动剂
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G蛋白偶联受体/G蛋白
帕金森与阿尔茨海默症
/ Glucagon Receptor / Exendin(9-39) amide/艾塞那肽 (9-39)

Exendin(9-39) amide/艾塞那肽 (9-39) {[allProObj[0].p_purity_real_show]}

货号：A365920 同义名： Avexitide; Exendin (9-39)

Exendin(9-39) amide是胰高血糖素样肽-1（GLP-1）受体的拮抗剂，也能抑制葡萄糖依赖性胰岛素分泌肽（GIP）受体结合。

Exendin(9-39) amide/艾塞那肽 (9-39) 化学结构 CAS号：133514-43-9
Exendin(9-39) amide/艾塞那肽 (9-39) 化学结构
CAS号：133514-43-9
Exendin(9-39) amide/艾塞那肽 (9-39) 3D分子结构
CAS号：133514-43-9
Exendin(9-39) amide/艾塞那肽 (9-39) 化学结构 CAS号：133514-43-9
Exendin(9-39) amide/艾塞那肽 (9-39) 3D分子结构 CAS号：133514-43-9
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Exendin(9-39) amide/艾塞那肽 (9-39) 纯度/质量文件 产品仅供科研

货号：A365920 标准纯度： {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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Exendin(9-39) amide/艾塞那肽 (9-39) 生物活性

描述 Glucagon-like peptide-1 (GLP-1) is a product of proglucagon cleavage synthesized in L cells in the intestinal mucosa, α-cells in the pancreatic islet, and neurons in the nucleus of the solitary tract. GLP-1 is released in response to nutrient absorption in the gut and helps to stimulate insulin secretion in the pancreaticb-cells while also suppressing glucagonsecretion[1]. 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. Exendin-(9-39) prevents hypoglycemia and maintains stability of blood glucose during a prolonged fast in individuals with KATPHI.[2]. It is an antagonist of the action of GLP-1(7-36) amide on arterial blood pressure and heart rate of rats. (3000ng of exendin 3-39 and 10ng of GLP-1 (7-36) amide)[3]. It inhibits exendin-3-induced increases in cAMP levels in guinea pig pancreas cells (IC50 = 20 nM)[4].

Exendin(9-39) amide/艾塞那肽 (9-39) 细胞实验

Cell Line
Concentration Treated Time Description References
CD34+ HSPCs 150 nM Used as a GLP-1R antagonist to block the effects of LIRA Cardiovasc Diabetol. 2022 Apr 9;21(1):51
hTRPV1-expressing CHO K1 cells 100 nM Inhibited CAP-induced TRPV1 calcium influx Exp Mol Med. 2024 Nov;56(11):2449-2464
Mouse DRG neurons 100 nM Inhibited CAP-induced TRPV1 inward currents and calcium responses Exp Mol Med. 2024 Nov;56(11):2449-2464

Exendin(9-39) amide/艾塞那肽 (9-39) 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Wild-type mice, Gcg null mice, GLP-1R KO mice, GcgRAΔvilcre mice, GcgRAΔPDX1Cre mice Intraperitoneal injection 50μg/100μl Single injection or 30-day continuous administration Ex9 impaired glucose tolerance in wild-type mice but had no impact on Gcg null or GLP-1R KO mice suggesting that Ex9 is a true and specific GLP-1R antagonist. Unexpectedly, Ex-9 had no effect on blood glucose in mice with restoration of intestinal Gcg. In contrast, pancreatic reactivation of Gcg fully restored the effect of Ex9 to impair both oral and IP glucose tolerance. Cell Metab. 2017 Apr 4;25(4):927-934. e3
Mice CAP-induced acute pain model Intraplantar injection 5 and 10 μg Single administration Alleviated CAP-induced spontaneous pain behaviors Exp Mol Med. 2024 Nov;56(11):2449-2464
Rats Myocardial infarction model Intravenous injection 50 mg/kg Single dose Blockade of GLP-1 receptors abolished the protective effects of remote ischemic preconditioning and perconditioning Cardiovasc Res. 2016 Dec;112(3):669-676
Mice GcgRAΔNull, GcgRAΔVilCre, GcgRAΔPDX1Cre mice Intraperitoneal injection 50 μg/100 μl Single dose Exendin-[9–39] (Ex9) was used as a GLP-1 receptor antagonist to evaluate the role of GLP-1 in the glucose-lowering effects of DPP-4 inhibitors. Results showed that Ex9 did not affect glucose tolerance in GcgRAΔNull and GcgRAΔVilCre mice but blunted the glucose-lowering effect of linagliptin in GcgRAΔPDX1Cre mice. Diabetologia. 2019 Oct;62(10):1928-1937

Exendin(9-39) amide/艾塞那肽 (9-39) 参考文献

[1]Doyle ME, Egan JM. Mechanisms of action of glucagon-like peptide 1 in the pancreas. Pharmacol Ther. 2007. 113:546–93.

[2]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. 61(10), 2585-91.

[3]Barragan J. M. et al. Interations of exendin-(9-39) with the effects of glucagon-like peptide-1-(-36) amide and of exendin-4 on arterial blood pressure and heart rate in rats. ELSEVIER. 1996. 67(1), 63-68.

[4]Ruffman, J.-P., Singh, L., and Eng, J. Exendin-3, a novel peptide from Heloderma horridum venom, interacts with vasoactive intestinal peptide receptors and a newly described receptor on dispersed acini from guinea pig pancreas. Description of exendin-3(9-39) amide, a specific exendin receptor antagonist. J. Biol. Chem. 1991. 266(5), 2897-2902.

Exendin(9-39) amide/艾塞那肽 (9-39) 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.30mL

0.06mL

0.03mL

1.48mL

0.30mL

0.15mL

2.97mL

0.59mL

0.30mL

Exendin(9-39) amide/艾塞那肽 (9-39) 技术信息

CAS号133514-43-9
分子式C149H234N40O47S
分子量 3369.76
SMILES Code C([C@H](NC([C@@H](NC([C@@H](NC([C@H](CC1=CC=CC=C1)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](CC(O)=O)N)=O)CC(C)C)=O)CO)=O)CCCCN)=O)CCC(N)=O)=O)CCSC)=O)CCC(O)=O)=O)CCC(O)=O)=O)CCC(O)=O)=O)C)=O)[C@@H](C)C)=O)CCCNC(=N)N)=O)CC(C)C)=O)=O)[C@H](CC)C)=O)CCC(O)=O)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(NCC(=O)N2[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(=O)N3[C@H](C(=O)N4[C@H](C(=O)N5[C@H](C(N[C@H](C(N)=O)CO)=O)CCC5)CCC4)CCC3)C)=O)=O)CO)=O)CO)=O)CCC2)=O)=O)CC(N)=O)=O)CCCCN)=O)CC(C)C)=O)C=6C=7C(NC6)=CC=CC7
MDL No. MFCD02179664
别名 Avexitide; Exendin (9-39); Exendin-3 (9-39) amide
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

H2O: 50 mg/mL(14.84 mM)，配合低频超声助溶

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Exendin(9-39) amide | 133514-43-9 | Avexitide | GCGR | GLP-1R Antagonist | GPCR/G Protein | GCGR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Exendin(9-39) amide/艾塞那肽 (9-39) 纯度/质量文件 | Exendin(9-39) amide/艾塞那肽 (9-39) 生物活性 | Exendin(9-39) amide/艾塞那肽 (9-39) 参考文献 | Exendin(9-39) amide/艾塞那肽 (9-39) 实验方案 | Exendin(9-39) amide/艾塞那肽 (9-39) 技术信息

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