Etelcalcetide CAS 1262780-97-1

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Etelcalcetide is a white or almost white crystalline powder, sometimes also a light yellow color. It is usually odorless and soluble in water. The chemical formula is C26H27N5O2, with a relative molecular weight of 445.531 g/mol. It is an antidepressant drug that is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of the serotonin 1A receptor. It has optical rotation, with a rotation angle of+30 ° to+35 ° (10mg/ml, in water). It is a chiral molecule that may form different enantiomers during chemical synthesis. Due to the presence of enantiomers, there may be differences in their optical rotation and other optical properties. The infrared spectrum shows characteristic absorption peaks, and the stretching vibration absorption peak of NH can be observed at approximately 3400 cm-1; A stretching vibration absorption peak of CH3 can be observed at approximately 2920 cm-1; A stretching vibration absorption peak of CO can be observed at approximately 1650 cm-1; A stretching vibration absorption peak of the aromatic ring can be observed at approximately 1500 cm-1.

Etelcalcetide is an effective oral dipeptidyl peptidase 4 (DPP-4) inhibitor, mainly used to treat type 2 diabetes. As a new type of anti diabetes drug, it has many functions, which are of great significance to improve the blood sugar control and life quality of diabetes patients.

1. Reduce blood sugar levels

The main function is to lower blood sugar levels. It reduces the degradation of glucagon like peptide-1 (GLP-1) and glucose dependent insulinotropic peptides (GIP) in the body by inhibiting the activity of DPP-4 enzyme, thereby increasing the physiological activity of these intestinal pro-insulins. GLP-1 and GIP can promote insulin secretion, inhibit the release of glucagon, and thereby lower blood sugar levels. This effect of Veracatide is helpful to improve the blood sugar control of diabetes patients and reduce the occurrence of complications.

2. Improve insulin resistance

Insulin resistance is one of the important pathophysiological characteristics of type 2 diabetes. Its substance improves insulin resistance by increasing insulin sensitivity. It can promote the uptake and utilization of insulin by adipocytes and muscle cells, enhance the biological activity of insulin, and thus enhance the body's sensitivity to insulin. This effect helps to reduce blood sugar levels and reduce the need for insulin in patients with diabetes.

3. Promotion β Cell regeneration and functional recovery

It also has the function of promoting pancreatic islets β The role of cell regeneration and functional recovery. By inhibiting the activity of DPP-4 enzyme, protection can be achieved β Cells are protected from damage factors such as high blood sugar and oxidative stress, promoting β The survival and proliferation of cells. In addition, it can also increase β The synthesis and secretion of intracellular insulin, improving β The functional activity of cells. These effects are helpful to improve the islet function of patients with diabetes and increase the level of insulin secretion.

4. Reduce weight and fat accumulation

It also has the effect of reducing weight and fat accumulation. It can reduce appetite and food intake, and lower energy intake. At the same time, veracalide can also promote the breakdown and metabolism of fat, reducing the accumulation of fat in the body. This effect can help to improve the obesity of diabetes patients and reduce the risk of cardiovascular disease and other complications.

5. Improve blood lipid metabolism

It can also improve blood lipid metabolism and lower blood lipid levels. It can increase the synthesis and secretion of high-density lipoprotein (HDL), and reduce the levels of low-density lipoprotein (LDL) and total cholesterol (TC). In addition, it can also inhibit the synthesis and accumulation of triglycerides, and reduce the level of triglycerides in plasma. These effects help reduce the risk of cardiovascular disease in patients with diabetes.

6. Protecting the cardiovascular system

It also has a protective effect on the cardiovascular system. It can lower blood pressure, reduce the occurrence of cardiovascular diseases such as heart hypertrophy and myocardial damage. In addition, it can also inhibit the inflammatory and oxidative stress responses of endothelial cells, protecting the health and integrity of blood vessel walls. These effects help to reduce the risk of cardiovascular disease in patients with diabetes and improve the quality of life.

7. Improve cognitive function

Recent studies have shown that it also has the effect of improving cognitive function. It can increase the content and activity of neurotransmitters in the brain, such as acetylcholine and dopamine, and improve the excitability and information transmission efficiency of neurons. In addition, it can also inhibit inflammation and oxidative stress reactions in the brain, protecting the health and survival of neurons. These effects are helpful to improve the cognitive dysfunction of diabetes patients and improve the quality of life.

8. Improve quality of life

In summary, by reducing blood sugar levels, improving insulin resistance, and promoting β Cell regeneration and functional recovery, weight reduction and fat accumulation reduction, lipid metabolism improvement, cardiovascular system protection, cognitive function improvement and other effects provide a comprehensive and effective treatment for diabetes patients. The exertion of these functions will help to improve the blood sugar control and quality of life of patients with diabetes, reduce the risk of complications, and improve the survival rate and health level of patients. Therefore, Veracatide has important clinical value and application prospect in the treatment of diabetes.

Etelcalcetide is a dipeptidyl peptidase 4 (DPP-4) inhibitor, which is mainly used to treat type 2 diabetes. Its synthesis involves multiple steps, and the following will provide a detailed introduction to its common laboratory synthesis methods and corresponding chemical equations.

Synthesis steps:

1. Activation of amino acids

Firstly, it is necessary to select appropriate amino acids for activation. The commonly used activation method is to activate carboxyl groups using N-hydroxysuccinimide (NHS) and N, N '- dicyclohexylcarbodiimide (DCC).

Chemical equation (using L-alanine as an example):

C₃H₇NO₂+C₄H₅NO₃+C₁₃H₂₂N₂ → C₃H₇NO₂NHS+C₁₃H₂₄N₂O

Among them, DCU is N, N '- dicyclohexylurea, which is a byproduct of the reaction.

2. Condensation reaction

The activated amino acid undergoes a condensation reaction with the amino group of the next amino acid to form a peptide bond. This step is usually carried out under alkaline conditions, such as using triethylamine as a base.

Chemical equation (using L-alanine and L-leucine as examples):

C₃H₇NO₂-NHS+C₆H₁₃NO₂+C₆H₁₅N → C₃H₇NO₂-L-C₆H₁₃NO₂+H₂O+NHS - triethylamine salt

3. Extension of peptide chains

By repeating the condensation reaction, gradually connect the required amino acids to the peptide chain until the complete sequence of veracalide is obtained.

4. Cyclization reaction

Veracapeptide molecules contain a specific cyclic structure that needs to be formed through cyclization reactions. This usually involves a reaction between one side chain group and another group on the peptide chain.

Chemical equation (using a simplified fragment of veracalide as an example):

H₂N peptide chain CO-R1+peptide chain CO-R2 → [H₂N peptide chain CO-R1] - peptide chain CO-R2+H₂O

R1 and R2 represent different functional groups on the peptide chain, forming a cyclic structure through reaction.

5. Purification and crystallization

After completing the cyclization reaction, the product needs to be purified and crystallized to obtain high-purity veracalide. This usually involves steps such as column chromatography, thin-layer chromatography, and recrystallization.

The development prospects of Etelcalcetide are very broad, mainly based on its significant therapeutic effects and unique mechanism of action in the medical field. The following is a detailed analysis of its development prospects:

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