GLP-1(7-37)
(Synonyms: 人胰高血糖素样肽-1) 目录号 : GC30058
GLP-1(7-37)是一种截短的胰高血糖素样肽，对GLP-1受体的EC50值为0.9 ± 0.1nM。
Cas No.:106612-94-6
Sample solution is provided at 25 µL, 10mM.
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GLP-1(7-37) is a truncated glucagon-like peptide with an EC50 value of 0.9 ± 0.1nM for GLP-1 receptors[1]. GLP-1(7-37) can bind to a specific GLP-1 receptor (GLP-1R) on pancreatic beta cells and enhance glucose-stimulated insulin secretion [2]. GLP-1(7-37) has been widely used as a model compound to develop a range of derivatives and GLP-1R agonists[3].
In vitro, GLP-1(7-37) treatment at 10nM for 30min significantly promoted cAMP generation as well as insulin secretion in Beta-TC-1 cells[4]. Pretreatment with 100nM GLP-1(7-37) for 3h enhanced the mitochondrial response to 25mM glucose stimulation in uninjured MitpHGV-MIN6 cells[5]. Treatment with 100nM GLP-1(7-37) for 10 seconds increased intracellular free calcium ions ([Ca2+]i) in COS-7 cells expressing the GLP-l receptor[6].
In vivo, GLP-1(7-37) treatment (5pmol/min/kg) via intravenous infusion (2h) into Zucker diabetic fatty (ZDF) rats transiently increased plasma insulin concentrations and normalized blood glucose concentrations[7]. Intravenous infusion of GLP-1(7-37) for 60 minutes (5pmol/min/kg) produced a transient increase in plasma insulin concentrations and a sustained slight decrease in blood glucose in fasted rats[8].
References:
[1] de Menthière C S, Chavanieu A, Grassy G, et al. Structural requirements of the N-terminal region of GLP-1-[7-37]-NH2 for receptor interaction and cAMP production[J]. European journal of medicinal chemistry, 2004, 39(6): 473-480.
[2] Vahl T P, Paty B W, Fuller B D, et al. Effects of GLP-1-(7–36) NH2, GLP-1-(7–37), and GLP-1-(9–36) NH2 on intravenous glucose tolerance and glucose-induced insulin secretion in healthy humans[J]. The Journal of Clinical Endocrinology & Metabolism, 2003, 88(4): 1772-1779.
[3] Manandhar B, Ahn J M. Glucagon-like peptide-1 (GLP-1) analogs: recent advances, new possibilities, and therapeutic implications[J]. Journal of medicinal chemistry, 2015, 58(3): 1020-1037.
[4] Fehmann H C, Habener J F. Functional receptors for the insulinotropic hormone glucagon‐like peptide‐I (7–37) on a somatostatin secreting cell line[J]. FEBS letters, 1991, 279(2): 335-340.
[5] Ogata M, Iwasaki N, Ide R, et al. GLP-1-related proteins attenuate the effects of mitochondrial membrane damage in pancreatic β cells[J]. Biochemical and Biophysical Research Communications, 2014, 447(1): 133-138.
[6] Wheeler M B, Lu M, Dillon J S, et al. Functional expression of the rat glucagon-like peptide-I receptor, evidence for coupling to both adenylyl cyclase and phospholipase-C[J]. Endocrinology, 1993, 133(1): 57-62.
[7] Hargrove D M, Nardone N A, Persson L M, et al. Glucose-dependent action of glucagon-like peptide-1 (7-37) in vivo during short-or long-term administration[J]. Metabolism, 1995, 44(9): 1231-1237.
[8] Hargrove D M, Nardone N A, Persson L M, et al. Comparison of the glucose dependency of glucagon-like peptide-1 (7–37) and glyburide in vitro and in vivo[J]. Metabolism, 1996, 45(3): 404-409.
GLP-1(7-37)是一种截短的胰高血糖素样肽，对GLP-1受体的EC50值为0.9 ± 0.1nM[1]。GLP-1(7-37)可通过与胰腺β细胞上的特异性GLP-1受体（GLP-1R）结合，增强葡萄糖刺激的胰岛素分泌[2]。GLP-1(7-37)作为模型化合物被广泛用于开发一系列衍生物和GLP-1R激动剂[3]。
在体外，10nM GLP-1(7-37)处理Beta-TC-1细胞30分钟可显著促进cAMP生成及胰岛素分泌[4]。100nM的GLP-1(7-37)预处理未受损的MitpHGV-MIN6细胞3小时能增强线粒体对25mM葡萄糖刺激的响应[5]。100nM的GLP-1(7-37)处理表达GLP-1受体的COS-7细胞10秒钟可增加细胞内游离钙离子（[Ca2+]i）浓度[6]。
在体内，Zucker糖尿病肥胖（ZDF）大鼠经静脉输注GLP-1(7-37)（5pmol/min/kg；持续2小时）可短暂升高血浆胰岛素浓度并使血糖浓度正常化[7]。禁食大鼠静脉输注GLP-1(7-37)（5pmol/min/kg；持续60分钟）能引起血浆胰岛素浓度瞬时升高及血糖持续轻度下降[8]。
| Cell experiment [1]: | |
Cell lines | Beta-TC-1 cell |
Preparation Method | Beta-TC-1 cells were grown in RPMI medium supplemented with 10% fetal bovine serum,5% horse serum, 100U/ml penicillin, and 100µg/ml streptomycin in a 95% O2, and 5% CO2 humidified atmosphere. Two days before the experiment, approximately 5×l05 cells were transferred to each well of 24-well plates. At the beginning of the cells were washed twice with KRB buffer and incubated in the medium (1ml) for 60min (37°C). Then, the buffer was changed to a buffer (300µl) containing the GLP-1(7-37) at 10nM for 30min. The entire supernatant was lyophilized and reconstituted in assay buffer for cAMP determination. |
Reaction Conditions | 10nM; 30min |
Applications | GLP-l(7-37) treatment promoted cAMP formation in Beta-TC-1 cells. |
| Animal experiment [2]: | |
Animal models | Zucker diabetic fatty (ZDF) rat |
Preparation Method | ZDF rats were housed in an environmentally controlled room (21°C with a 12-hour light/dark cycle) with food (standard rodent chow) and water available ad libitum. Fed ZDF rats were intravenously infused for 2 hours with GLP-1(7-37) at 5pmol/min/kg. Blood samples were taken from the carotid artery catheter every 15 minutes for plasma glucose and at 0, 15, 30, 60, and 120 minutes for determinations of insulin. |
Dosage form | 5pmol/min/kg for 2h; i.v. |
Applications | GLP-l(7-37) treatment increased plasma insulin concentration and normalized the plasma glucose concentration in rats. |
References: | |
| Cas No. | 106612-94-6 | SDF | |
| 别名 | 人胰高血糖素样肽-1 | ||
| Canonical SMILES | His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-Gly | ||
| 分子式 | C151H228N40O47 | 分子量 | 3355.67 |
| 溶解度 | Water : 30 mg/mL (8.94 mM) | 储存条件 | Store at -20°C,protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 298 μL | 1.49 mL | 2.98 mL |
| 5 mM | 59.6 μL | 298 μL | 596 μL |
| 10 mM | 29.8 μL | 149 μL | 298 μL |
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