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Exenatide Acetate is a peptide drug that is a white to grayish white powder with almost no odor. Molecular formula C186H286N50O62S, CAS 141732-76-5. Soluble in organic solvents such as water, methanol, and DMSO. The solubility in water is relatively high, which provides convenience for the preparation of formulations in solution form. At room temperature, it is relatively stable. However, high temperatures may affect its stability and lead to decomposition. Therefore, it is necessary to store and transport product under appropriate temperature and humidity conditions. It belongs to GLP-1 receptor agonist and is used to treat type 2 diabetes.
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Exenatide Acetate has a variety of applications, mainly concentrated in the fields of diabetes treatment and biomedical research. The following is a specific introduction:
Diabetes Treatment
Exenatide is a glucagon-like peptide-1 (GLP-1) analogue. By simulating the physiological effects of GLP-1, it promotes glucose-dependent insulin secretion, inhibits inappropriate glucagon secretion, slows down gastric emptying, thereby improving the sensitivity of peripheral tissues to insulin and achieving the effect of lowering blood sugar.
Clinical application
It is suitable for type 2 diabetic patients whose blood glucose is not well controlled despite the use of metformin alone, sulfonylureas, or the combination of metformin and sulfonylureas. Studies have shown that exenatide can reduce fasting and postprandial blood glucose concentrations in patients with type 2 diabetes and improve blood glucose control.
Pharmacological characteristics
It only causes insulin release when glucose concentration rises. When blood glucose concentration drops and approaches normal levels, insulin secretion decreases, thereby reducing the risk of hypoglycemia.
Restoring the first-phase insulin response
Patients with type 2 diabetes typically lack the first-phase insulin response (a large amount of insulin is secreted within 10 minutes after intravenous glucose injection). Exenatide acetate can restore this response and enhance the responsiveness of pancreatic β cells to glucose.
During hyperglycemia, reduce glucagon secretion, lower serum glucagon concentration, decrease hepatic glucose output, reduce insulin demand, and at the same time, do not damage the normal glucagon response to hypoglycemia.
Slow down gastric emptying
Slowing down the rate at which glucose from food enters the circulation helps stabilize blood sugar fluctuations.
Biomedical Research
Fluorescently labeled derivatives of Exenatide (such as CY5-Exenatide acetate) can be used to study its distribution and metabolic process in vivo, providing an important basis for drug research and development and optimization.
Receptor binding studies:
Exenatide, as a polypeptide compound, can bind to specific receptors and is suitable for molecular pharmacological research. By studying its binding characteristics with target receptors, one can gain an in-depth understanding of its mechanism of action and signal transduction pathways.
Biological imaging
Cy5-exenatide Acetate: An Exenatide derivative labeled with CY5 fluorescent dye, suitable for biomolecular research, receptor binding analysis and bioimaging experiments. The red fluorescence characteristics of CY5 (excitation wavelength approximately 649 nm, emission wavelength approximately 670 nm) enable it to have a high signal-to-noise ratio and low background interference in fluorescence microscopy, flow cytometry and in vivo imaging experiments.
Application fields: It is suitable for confocal fluorescence microscopy, fluorescence-activated cell sorting (FACS), and fluorescence resonance energy transfer (FRET) experiments, and can be used to study the distribution of exenatide in cells, receptor interactions, and metabolic processes.
Cell uptake research:
Studying the uptake and distribution of exenatid in different cell types is helpful for understanding its pharmacokinetic characteristics and mechanism of action in vivo.
Exenatide acetate has a wide range of uses and involves many aspects, so how to improve its synthesis efficiency has become a concern for many researchers. In the following text, we will introduce a synthetic route proposed by our researchers.
Step 1: Synthesize Fmoc Gly Pro Se (tBu) Se (tBu) Gly Ala Pro Pro Se (tBu) - MBHA Resin
1) Synthesis of Fmoc Ser (tBu) - MBHA Resin
After swelling Fmoc Rink Amide MBHA Resin with N, N-dimethylformamide, remove Fmoc twice with a mixture of piperidine and N, N-dimethylformamide in a volume ratio of 1:4. Add N, N-dimethylformamide, Fmoc Ser (tBu) - OH, 1-hydroxyphenylpropanetriazole, benzotriazole-N, N, N ', N' - tetramethylurea tetrafluoroboric acid, N, N '- diisopropylethylamine, and stir at room temperature for 1-3 hours under nitrogen protection, Obtain Fmoc Ser (tBu) - MBHA Resin.
2) Synthesis of Fmoc Pro Se (tBu) - MBHA Resin
Fmoc Ser (tBu) - MBHA Resin was removed twice using a mixture of piperidine and N, N-dimethylformamide in a volume ratio of 1:. N, N-dimethylformamide, Fmoc Pro OH, 1-hydroxyphenylpropanetriazole, benzotriazole-N, N, N ', N' - tetramethylurea tetrafluoroboric acid, N, N '- diisopropylethylamine were added, and stirred at room temperature for 1-3 hours under nitrogen protection to obtain Fmoc Pro Ser (tBu) - MBHA Resin.
3) Synthesis of Fmoc Gly Pro Se (tBu) Se (tBu) Gly Ala Pro Pro Se (tBu) - MBHA Resin
Connect Fmoc Pro OH, Fmoc Pro OH, Fmoc Ala OH, Fmoc Gly OH, Fmoc Ser (tBu) OH, Fmoc Ser (tBu) OH, Fmoc Pro OH, and Fmoc Gly OH to Fmoc Pro Se (tBu) Se (tBu) - Gly Ala Pro Pro Se (tBu) - MBHA Resin in sequence according to step (2), to obtain Fmoc Gly Pro Se (tBu) - Gly Ala Pro Se (tBu) - MBHA Resin.
Step 2: Synthesize Fmoc Lys (Boc) - Asn (Trt) - Gly COOH
1) Synthesis of Fmoc Gly-2-CTC resin
After swelling 2-chlorotrityl chloride resin with dichloromethane, add dichloromethane, Fmoc Gly-OH, N, N '- diisopropylethylamine, and stir at room temperature for 1-3 hours under nitrogen protection to obtain Fmoc Gly-2-CTC resin.
2) Synthesis of Fmoc Lys (Boc) - Asn (Trt) - Gly-2-CTC resin
Following the method in step 1 (2), connect Fmoc Asn (Trt) - OH and Fmoc Lys (Boc) - OH sequentially to Fmoc Gly-2-CTC resin to obtain Fmoc Lys (Boc) - Asn (Trt) - Gly-2-CTC resin.
3) Cutting treatment
Add cutting fluid to Fmoc Lys (Boc) - Asn (Trt) - Gly-2-CTC resin, stir at room temperature for 1-3 hours, filter, add the filtrate to cold ether, precipitate, and obtain Fmoc Lys (Boc) - Asn (Trt) - Gly COOH. The cutting fluid mentioned above is a mixture of trifluoroacetic acid and dichloromethane in a volume ratio of 1:99 or 2:98, or a mixture of trifluoroethanol and acetic acid and dichloromethane in a volume ratio of 2:1:7.
Step 3: Synthesize Fmoc Val Arg (pbf) - Leu The Ile Glu (otBu) - Trp Leu COOH
Following the method in step 2 (1), connect Fmoc Leu OH to the 2-chlorotrityl chloride resin to obtain Fmoc Leu 2-CTC resin.
Then, follow the method in step 2 (2) to sequentially connect Fomc Trp OH, Fmoc Glu (otBu) OH, Fmoc Ile OH, Fmoc Phe OH, Fmoc Leu OH, Fmoc Arg (pbf) OH, Fomc Val Arg (pbf) - Leu He Ile Glu (otBu) - Trp Leu-2-CTC Resin, Fmoc Val Arg (pbf) - Leu The Ile Glu (otBu) - Trp Leu-2-CTC Resin was cut according to the method in step 2 (3) to obtain Fmoc Val Arg (pbf) - Leu The Ile Glu (otBu) - Trp Leu COOH.
Step 4: Synthesize Fmoc Met Glu (otBu) - Glu (otBu) - Glu (otBu) - Ala COOH
Following the method in step 2 (1), connect Fomc Ala-OH to the 2-chlorotrityl chloride resin to obtain Fmoc Ala-2-CTC resin.
Then, follow the method in step 2 (2) to connect Fomc Glu (otBu) - OH, Fmoc Glu (otBu) - OH, Fmoc Glu (otBu) - OH, Fomc Met Glu (otBu) - Glu (otBu) - Glu (otBu) - Glu (otBu) - A la-2-CTC Resin, Fmoc Met Glu (otBu) - Glu (otBu) - Glu (otBu) - Ala-2-CTC Resin was cut according to the method in step 2 (3) to obtain Fmoc Met Glu (otBu) - Glu (otBu) - Glu (otBu) - Ala-COOH.
Step 5: Synthesize Fmoc Thr (tBu) - Se (tBu) - Asp (otBu) - Leu Se (tBu) - Lys (Boc) - Gln (Trt) - COOH
Following the method in step 2 (1), connect Fomc Gln (Trt) - OH to the 2-chlorotrityl chloride resin to obtain Fmoc Gln (Trt) -2-CTC resin.
Then, follow the method in step 2 (2) to sequentially connect Fomc Lys (Boc) - OH, Fmoc Ser (tBu) - OH, Fmoc Leu OH, Fmoc Asp (otBu) - OH, Fmoc Ser (tBu) - OH, Fomc Thr (tBu) - OH) to the Fmoc Gln (Trt) -2-CTC resin. tBu) - OH, Obtain Fmoc Thr (tBu) - Ser (tBu) - Asp (otBu) - Leu Ser (tBu) - Lys (Boc) - Gln (Trt) -2-CTC Resin, Fmoc Thr (tBu) - Ser (tBu) - Asp (otBu) - Leu Ser (tBu) - Lys (Boc) - Gln (Trt) -2-CTC Resin, and perform cutting and processing according to the method in step 2-3 to obtain Fmoc Thr (tBu) - Ser (tBu) - Asp (otBu) - Leu Ser (tBu) -2-CTC Resin. -Lys (Boc)-Gln (Trt)-COOH.
Step 6: Synthesize Fmoc His (Trt) Gly Glu (otBu) Gly Thr (tBu)-He COOH
Following the method in step 2 (1), connect Fomc Phe OH to the 2-chlorotrityl chloride resin to obtain Fmoc Phe-2-CTC resin.
Then, follow the method in step 2 (2) to sequentially connect Fomc Tyr (tBu) OH, Fmoc Gly OH, Fmoc Glu (otBu) OH, Fmoc Gly OH, Fomc His (Trt) - OH to the Fmoc Phe-2-CTC resin, Obtain Fmoc His (Trt) - Gly Glu (otBu) - Gly Glu (tBu) - Phe-2-CTC ResinFmoc His (Trt) - Gly Glu (otBu) - Gly Tyr (tBu) - Phe-2-CTC Resin and perform cutting treatment according to the method in step 2 (3) to obtain Fmoc His (Trt) - Gly Glu (otBu) - Gly Tr (tBu) - Phe-COOH.
Step 7: Synthesize exenatide
1) Assemble and connect Fmoc Lys (Boc) - Asn (Trt) - Gly Gly Pro Se (tBu) - Se (tBu) - Gly Ala Pro Pro Pro Se (tBu) - MBHA Resin
Remove Fmoc Gly Pro Se (tBu) Se (tBu) Gly Ala Pro Pro Pro Se r (tBu) MBHA Resin obtained from step 1 twice using a mixture of piperidine and N, N-dimethylformamide in a volume ratio of 1:4. Add a mixture of N, N-dimethylformamide and dimethyl sulfoxide, N-methylpyrrolidone in a volume ratio of 0.5-1:1:2:1, as well as Fmoc Lys (Boc) Asn (Trt) Gly COOH, 1-hydroxyphenylpropanetriazole, benzotriazole-N, N, N ', N '- tetramethylurea tetrafluoroborate and N, N' - diisopropylethylamine were stirred at room temperature for 3-4 hours under nitrogen protection to obtain Fmoc Lys (Boc) - Asn (Trt) - Gly Gly Pro Se (tBu) - Se (tBu) - Gly Ala Pro Pro Ser (tBu) - MBHA Resin.
2) Assembly and connection of exenatide
According to the assembly and connection method in step (1), sequentially assemble and connect Fmoc Val Arg (pbf) - Le Glu (otBu) - Trp Leu COOH, Fmoc Met Glu (otBu) - Glu (otBu) - Glu (otBu) - Glu (otBu) - Glu (otBu) - Ala COOH, Fmoc Thr (tBu) - Se (tBu) - Asp (otBu) - Le Se (tBu) - Lys (Boc) - Gln (Trt) - COOH, Fmoc His (Trt) - Gly Glu (otBu) - Gly Thr (tBu) - PheCOOH, Using a mixture of piperidine and N, N-dimethylformamide in a volume ratio of 1:4, Fmoc was removed twice to obtain exenatide resin.
Using a cutting solution composed of 83% trifluoroacetic acid, 5% phenol, 4% benzyl sulfide, 3% water, and 5% triisopropylsilane by mass percentage, the resin of exenatide was cut according to the method in step (2) to obtain crude exenatide. The crude exenatide was purified by reverse phase chromatography and freeze-dried to obtain Exenatide acetate.
Frequently Asked Questions
Is exenatide the same as metformin?
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In conclusion, for an initial therapy in overweight/obese patients with newly diagnosed T2D, exenatide causes a better glycemic control than metformin, whose mechanism might potentially be related to the better weight loss effect and amelioration of β-cell function.
Is exenatide FDA approved?
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Exenatide (brand name Byetta) was first approved by the FDA on April 28, 2005, as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It is a GLP-1 receptor agonist, with later formulations including once-weekly extended-release (Bydureon) approved in 2012, and pediatric approval for ages 10+ in 2021.
How to get exenatide?
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Bydureon (exantide) is an extended-release injectable diabetes medication that helps control blood sugar. Extended-release exenatide helps the pancreas produce insulin more efficiently. Bydureon treats type 2 diabetes mellitus in combination with diet and exercise. Bydureon is available only by prescription.
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