Retatrutide

Ретатрутид

Ретатрутид

Retatrutide is a revolutionary peptide targeting three key metabolic receptors.

 

Артикул: 198881 Категория:
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Retatrutide is a new triple-receptor agonist peptide originated from the GLP-1-based dual agonist Tirzepatide. It selectively targets three key metabolic receptors: the glucagon receptor (ГКГР), the glucose-dependent insulinotropic polypeptide receptor (GIPR), и рецептор глюкагоноподобного пептида-1 (ГЛП-1Р). This new peptide drug shows strong potential in treating obesity-related metabolic disorders and type 2 diabetes due to its unique structure.

Более того, Scientists developed Retatrutide peptide on an optimized GLP-1 analog scaffold and it consists of 39 аминокислоты. Its sequence incorporates three non-natural amino acids to enhance resistance to degradation by dipeptidyl peptidase-4 (DPP-4). Более того, the introduction of AIB (2-Aminoisobutyric acid) significantly improves both biological activity and pharmacokinetics.

Кроме того, the attachment of a C20 fatty diacid chain a лизин residue extends its период полураспада and improves its pharmacological profile. Вместе, these advanced features support once-weekly subcutaneous dosing.

Последовательность

Tyr-{Аиб}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{α-Me-Leu}-Leu-Asp-Lys-{diacid-C20-gamma-Glu-(AEEA)-Лис}-Ala-Gln-{Аиб}-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

Номер CAS

2381089-83-2

Молекулярная формула

C221H342N46O68

Молекулярный вес

4731.33 г/моль

Research Of Retatrutide Benefits

1. Suppresses Appetite, Delays Gastric Emptying, and Stimulates Insulin

1)Mechanism of Action in Appetite Control

In an animal study, researchers fasted male obese mice для 16 hours and treated them with long-acting glucagon receptor agonists, Ретатрутид, galectin peptides, and other GLP-1 analogs for weight management. The study evaluated gastric emptying (GE) delay, body weight, and food intake.

2)Glucose-Dependent Gastric Emptying Delay:

Примечательно, Retatrutide delayed GE in a glucose-dependent manner. В частности, the group receiving 10 nmol/L Retatrutide showed the highest reduction in body weight and the largest decrease in food consumption.

3)Central Nervous System Effects:

Similarly to other GLP-1 receptor agonist, Retatrutide acts directly on the central nervous system, enhancing satiety and slowing gastric emptying. Как результат, it supports effective obesity treatment.

4)Clinical Trial Weight Loss Results:

Например, a Phase 2 clinical trial reported significant weight loss in overweight and obese adults: 17.5% в 24 weeks and 24.4% в 48 недели.

2. Treats Type 2 Диабет

  • A Phase 1b multiple ascending-dose study involved type 2 diabetes patients receiving weekly doses of Retatrutide or other glucose-lowering drugs, with a control group receiving no treatment.
  • Remarkably, Retatrutide achieved 100% of the weight loss target, compared to only 2.1% in the control group. В отличие, no other diabetes drug reached 50% эффективность.
  • These findings clearly demonstrate Retatrutide’s superior effectiveness in managing type 2 диабет. Однако, the most common side effects were gastrointestinal.
  • В то же время, in obese adults, Retatrutide treatment also led to significant weight loss over 48 недели.

3. Promotes Energy Expenditure

  • As a triple agonist, Retatrutide activates the glucagon receptor similarly to glucagon. Конкретно, it directly stimulates thermogenesis and fat breakdown.
  • It is important to note that glucagon receptors are present in the liver and жировая ткань. By activating these receptors, Retatrutide increases energy expenditure and heat production in the liver.
  • Следовательно, it boosts metabolic rate and promotes fat oxidation.

4. Reduces Inflammation and Treats Fatty Liver Disease

1)Anti-Inflammatory Benefits

Retatrutide offers multi-faceted anti-inflammatory benefits. Например, studies show it improves glucose tolerance, reduces body weight and fat mass, and enhances lipid profiles.

2)Reversal of Steatohepatitis in Mice

Кроме того, it reverses steatohepatitis in female mice, supporting resolution of fatty liver disease by reducing hepatic steatosis. In one study, mice that researchers fed a high-fat, high-sugar diet for 38 weeks received subcutaneous Retatrutide, and researchers fasted them for 4 часы.

Впоследствии, histological analysis showed over 80% had definite steatohepatitis. Importantly, Retatrutide improved the condition dose-dependently, with some females showing complete reversal.

3)Histological Analysis Results

In another human trial, researchers treated 98 participants with ≥10% liver fat content. После 48 weeks of Retatrutide treatment, liver fat decreased by 51.3% (1 мг), 59% (4 мг), и 86% (12 мг), по сравнению с 4.6% in the control group.

В конечном счете, all treated patients achieved normal liver fat levels.

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