Tirzepatide Hypoglycemic Drugs

English name：Tirzepatide
CAS number：2023788-19-2
Molecular formula: C225H348N48O68
Molecular weight: 4813
EINECS number: 200-001-8

Related category
Polypeptide; Small molecule inhibitor; Catalog peptide; Polypeptide; Drug polypeptide; Beauty polypeptide; Drug peptide; Pharmaceutical raw materials; Others; New products; APIs; API; Belka staple
Mol file：2023788-19-2.mol
 

Structural formula:

Properties of tilpotide

Storage: Store at -20°C

Solubility: Dissolved in dimethyl sulfoxide

Form: solid

Color: White to beige

Sequence：Tyr-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{Aib}-Leu-Asp-Lys-Ile-Ala-Gln-{diacid-C20-gamma-Glu-(AEEA)2-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

Hypoglycemic drugs

tirzepatide (tirzepatide) is a novel glucagon-like peptide-1 receptor (GLP-1) and glucose-dependent insulin-stimulating polypeptide (GIP, also known as gastric inhibitory polypeptide) double-receptor agonist administered once a week. Both GLP-1 and GIP belong to incretin, which is a polypeptide secreted by the gastrointestinal mucosa. The former can bind to the receptors on islet cells and stimulate the secretion of islet Chemicalbook, thus producing hypoglycemic effect, delaying gastric emptying and inhibiting appetite, thus controlling body weight. The latter has the function of inhibiting gastric acid, pepsin secretion, stimulating insulin release, inhibiting gastric peristalsis and emptying, and can supplement the effect of GLP-1 receptor agonist. tirzepatide combines the effects of two insulin-promoting drugs into a single molecule and represents a new class of drugs for the treatment of type 2 diabetes.

The molecule consists of a peptide skeleton of 39 amino acids and a side chain at Lys20. Of the 39 amino acids, 37 are naturally occurring (or coded) and two are non-naturally occurring, non-coding amino isobutyric acid residues at positions 2 and 13.

Use

Tirzepatide has a similar sequence to semaglutide, and the lys side chain in the sequence has PEG modification, which is the functional group of the polypeptide, and can increase the water solubility of the sequence. The main physiological function of TirzepChemicalbookatide is glucose-dependent insulin nutrition polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor double agonist, which is being developed for the treatment of type 2 diabetes and has entered the clinical stage.

Security

The safety profile of tilpotide is similar to that of other incretin drugs. A meta-analysis of seven randomized controlled trials showed that telpotide had significantly higher gastrointestinal reactions (such as nausea, diarrhea, and constipation) than Amicalbook, but most were mild to moderate. Other adverse reactions, especially hypoglycemia, were not significantly different between the two groups. However, due to the short listing time, the actual safety still needs to be displayed after listing.

Hypoglycemic and weight loss effects

SURPASS studies are a series of large clinical randomized controlled trials designed to evaluate the efficacy and safety of telpotide in patients with type 2 diabetes mellitus (T2DM). The head to head comparison with Semaglutide SURPASS 2[1] is the most exciting, comparing Tipotide 5mg (n=470), 10mg (n=469), and 15mg (n=469) with semaglutide 1mg (n=468) for glucose-lowering Chemicalbook. Telpotide reduced HbA1c by an average of 2.0%, 2.2%, and 2.3% compared with baseline HbA1c (8.3%), while semaglutide reduced Hba1c by an average of 1.9%. In terms of weight loss, telpotide resulted in average weight loss of 17, 21, and 25 pounds compared to baseline weight (207 pounds), compared with 13 pounds for semaglutide. The experiment showed that tilpotide showed better hypoglycemic and weight loss ability than semaglutide.

Another large study enrolled 2,539 adults with at least one obesity complication (excluding diabetes) with a body mass index (BMI) of ≥30kg/m2 or ≥27kg/m2. All subjects were randomly divided into Tipotide Chemicalbook5mg, 10mg, 15mg and placebo groups in equal proportion. The results showed that the body weight of each group decreased by 16.1kg, 22.2kg, 23.6kg and 2.4kg, respectively, at 72 weeks [2]. The weight loss effect of tilpotide is comparable to that of weight loss surgery.

Polypeptide

Tilpotide has a similar sequence to semaglutide. The lys side chain in the sequence has PEG modification, which is the functional group of polypeptide and can increase the water solubility of the sequence. Telpotide's main Chemicalbook physiological function is glucose-dependent insulin nutritional polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor double agonist, which is being developed for the treatment of type 2 diabetes and has entered the clinical stage.

Reference quality standard

Appearance: White powder

Purity (HPLC) : ≥95.0%

Acetic acid content: 5.0% ~ 12.0%

Moisture content: ≤8.0%

Peptide content: ≥70.0%

Amino acid composition analysis: ≤±10%

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