Exenatide acetate
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Exenatide acetate

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Exenatide acetate is a potent peptide agonist of the glucagon-like peptide 1 (GLP-1) receptor with Ki value of 136 pM. It is a 39 amino acid peptide, which increases intracellular cAMP in pancreatic acinar cells and has no effect on VIP receptors. It was first isolated from the venom of H. horridum and consequently synthesized. It stimulates proliferation of HCAECs through PKA-PI3K/Akt-eNOS activation pathways via a GLP-1 receptor-dependent mechanism. It also stimulates glucose-induced insulin secretion in isolated rat islets and proinsulin expression in mouse insulinoma βTC-1 cells. It protects hippocampal neurons against glutamate-induced apoptosis, suggesting utility in neurodegenerative diseases. It also has anxiolytic and anti-depressant effects and induces satiety. It is an incretin mimetic approved for type 2 diabetes mellitus treatment. It also has neurotrophic/protective activity in cellular and animal models of stroke, Alzheimer's and Parkinson's diseases.

Peptide Inhibitors
Catalog number
CAS number
Molecular Formula
Molecular Weight
Exenatide acetate
Size Price Stock Quantity
100 mg $899 In stock
1 g $2799 In stock
acetic acid;(4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]acetyl]amino]-5-oxopentanoic acid
L-Serinamide, L-histidylglycyl-L-α-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-α-aspartyl-L-leucyl-L-seryl-L-lysyl-L-glutaminyl-L-methionyl-L-α-glutamyl-L-α-glutamyl-L-α-glutamyl-L-alanyl-L-valyl-L-arginyl-L-leucyl-L-phenylalanyl-L-isoleucyl-L-α-glutamyl-L-tryptophyl-L-leucyl-L-lysyl-L-asparaginylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl-L-prolyl-, acetate (1:x); Exendin 4 (Heloderma suspectum), acetate; Exendin-4 acetate; H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-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.CH3CO2H
Related CAS
141758-74-9 (free base)
Solid powder
Store at -20°C
Soluble in DMSO (10 mM)
InChI Key
Canonical SMILES
1. Effect of water on exenatide acylation in poly(lactide-co-glycolide) microspheres
Rongcai Liang, Xiang Li, Yanan Shi, Aiping Wang, Kaoxiang Sun, Wanhui Liu, Youxin Li Int J Pharm. 2013 Sep 15;454(1):344-53. doi: 10.1016/j.ijpharm.2013.07.012. Epub 2013 Jul 16.
Peptide or protein degradation often occurs when water flows into the dosage form. The aim of this study was to investigate the effect of water on exenatide acylation in poly(lactide-co-glycolide) (PLGA) microspheres. Exenatide-loaded PLGA microspheres were incubated at different relative humidities (RH) as well as in solutions of different pH for 20 days. The stability of exenatide was monitored using HPLC and HPLC-MS analysis. The alteration of exenatide conformation caused by water was investigated by FT-IR spectroscopy. Exenatide and glycolide were incubated in DMSO-water solutions to verify the effect of exenatide conformation state on the peptide acylation. Exenatide was relatively stable in microspheres at lower RH, and the absorbed water could act as a plasticizer and thus promote the peptide acylation by PLGA. However, when the microspheres were incubated at 100% RH, the excessively absorbed water could cause conformation recovery of exenatide and play an inhibitory effect on acylation. The formation of acylated exenatide incubated in acetate buffer saline of pH 6.0 was more than that of pH 4.5 and 3.0. Stability studies of exenatide in glycolide solutions showed that exenatide in nonnative monomer state was easier to be acylated by eletrophiles than that in aggregation state.
2. [D-Leu-4]-OB3, a synthetic peptide amide with leptin-like activity, augments the effects of orally delivered exenatide and pramlintide acetate on energy balance and glycemic control in insulin-resistant male C57BLK/6-m db/db mice
Matthew C Leinung, Patricia Grasso Regul Pept. 2012 Nov 10;179(1-3):33-8. doi: 10.1016/j.regpep.2012.08.006. Epub 2012 Sep 5.
The escalation predicted for the incidence of both type 2 diabetes mellitus and obesity has prompted investigators to search for additional pharmacotherapeutic approaches to their treatment. Two of these approaches, combination pharmacotherapy and utilization of leptin-related bioactive synthetic peptides as anti-diabetes/anti-obesity agents, were used in the present study. Exenatide or pramlintide acetate was reconstituted in dodecyl maltoside (DDM) in the absence or presence of [D-Leu-4]-OB3, and delivered orally by gavage to insulin-resistant male C57BLK/6-m db/db mice twice daily for 14 days. Body weight gain, food and water intake, blood glucose, and serum insulin levels were measured. Mice given DDM alone for 14 days were 19.7% heavier than they were at the beginning of the study, while oral delivery of exenatide or [D-Leu-4]-OB3 in DDM reduced body weight gain to only 13.9% and 11.5%, respectively, of initial body weight. Mice receiving exenatide and [D-Leu-4]-OB3 were 4.2% lighter than they were at the beginning of the study. In another study, Intravail® treated control mice gained 38.2% of their initial body weight, while mice receiving pramlintide acetate or [D-Leu-4]-OB3 were only 26.8% and 25.4% heavier, respectively, at the end of the study, Co-administration of pramlintide acetate and [D-Leu-4]-OB3 did not further enhance the effect of pramlintide acetate on body weight gain. Food intake was reduced by exenatide, pramlintide acetate, and [D-Leu-4]-OB3 alone, and co-delivery with [D-Leu-4]-OB3 did not induce a further decrease. Water intake was not affected by exenatide, pramlintide acetate, or [D-Leu-4]-OB3 alone, but co-delivery of exenatide or pramlintide acetate with [D-Leu-4]-OB3 resulted in a significant reduction in water intake. Oral delivery of exenatide or pramlintide acetate in DDM significantly lowered blood glucose levels by 20.4% and 30.2%, respectively. Co-delivery with [D-Leu-4]-OB3 further reduced blood glucose by 38.3% and 50.5%, respectively. A concentration-dependent increase in serum insulin was observed in response to increasing concentrations of exenatide, and [D-Leu-4]-OB3 slightly reduced the insulin response to exenatide at all concentrations tested. Increasing concentrations of pramlintide acetate alone did not elevate serum insulin, and when given in combination with [D-Leu-4]-OB3, serum insulin levels fell below those of DDM-treated control mice. Our data indicate that (1) exenatide and pramlintide acetate, currently administered by subcutaneous injection, can be given orally in DDM; (2) the bioactivity of exenatide and pramlintide acetate is retained following oral delivery in DDM; and (3) the effects of exenatide and pramlintide acetate on energy balance and glycemic control can be enhanced by co-administration with [D-Leu-4]-OB3, a synthetic peptide amide with leptin-like activity.
3. Stability of exenatide in poly(D,L-lactide-co-glycolide) solutions: a simplified investigation on the peptide degradation by the polymer
Rongcai Liang, Renyu Zhang, Xiang Li, Aiping Wang, Daquan Chen, Kaoxiang Sun, Wanhui Liu, Youxin Li Eur J Pharm Sci. 2013 Nov 20;50(3-4):502-10. doi: 10.1016/j.ejps.2013.08.014. Epub 2013 Aug 29.
A solution model can be used to elucidate drug stability issues in a complex system. The aim of this study was to investigate the interaction between poly(D,L-lactide-co-glycolide) (PLGA) and exenatide in organic solvent-acetate buffer saline (ABS) solutions. The effect of solvent composition on exenatide stability was investigated first. In the selected 90:10 dimethyl sulfoxide (DMSO):ABS solution, exenatide stability was examined as a function of PLGA comonomer ratios, molecular weight (Mw) and concentrations. The specific rotation analysis and second derivative UV absorbance spectroscopy were used to monitor the variation of exenatide higher order structure. The effect of ABS pH on the interaction was also investigated. Exenatide degradation products were characterized by HPLC-MS/MS. It was found that exenatide was relatively stable in glacial acetic acid (HAc)-ABS solutions, whereas DMSO content had a strong influence on the conformation state and stability of exenatide. PLGA 50:50 promoted exenatide degradation more than PLGA 75:25 and poly(D,L-lactide) (PLA). Lower Mw and higher concentration of PLGA were beneficial for exenatide degradation. Exenatide was more stable in 90:10 DMSO:ABS (pH 3.0) solution than in 90:10 DMSO:ABS (pH 4.5 and 3.0) solutions during the incubation. HPLC-MS/MS analysis of exenatide demonstrated that acylation was the main degradation route of the peptide.
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