Retatrutide

Retatrutide

Retatrutide

Retatrutide is a revolutionary peptide targeting three key metabolic receptors.

 

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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 (GCGR), the glucose-dependent insulinotropic polypeptide receptor (GIPR), 그리고 글루카곤 유사 펩티드-1 수용체 (GLP-1R). This new peptide drug shows strong potential in treating obesity-related metabolic disorders and type 2 diabetes due to its unique structure.

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

추가적으로, the attachment of a C20 fatty diacid chain a 라이신 residue extends its 반감기 and improves its pharmacological profile. 함께, these advanced features support once-weekly subcutaneous dosing.

순서

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

CAS 번호

2381089-83-2

분자식

C221H342N46O68

분자량

4731.33 g/몰

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 ~을 위한 16 hours and treated them with long-acting glucagon receptor agonists, Retatrutide, 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:

특히, Retatrutide delayed GE in a glucose-dependent manner. 특히, 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. 결과적으로, it supports effective obesity treatment.

4)Clinical Trial Weight Loss Results:

예를 들어, a Phase 2 clinical trial reported significant weight loss in overweight and obese adults: 17.5% ~에 24 weeks and 24.4% ~에 48 주.

2. Treats Type 2 당뇨병

  • 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. 대조적으로, no other diabetes drug reached 50% efficacy.
  • These findings clearly demonstrate Retatrutide’s superior effectiveness in managing type 2 당뇨병. 하지만, the most common side effects were gastrointestinal.
  • 동시에, in obese adults, Retatrutide treatment also led to significant weight loss over 48 주.

3. Promotes Energy Expenditure

  • As a triple agonist, Retatrutide activates the glucagon receptor similarly to glucagon. 구체적으로, it directly stimulates thermogenesis and fat breakdown.
  • It is important to note that glucagon receptors are present in the liver and 지방 조직. By activating these receptors, Retatrutide increases energy expenditure and heat production in the liver.
  • 따라서, 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. 예를 들어, studies show it improves glucose tolerance, reduces body weight and fat mass, and enhances lipid profiles.

2)Reversal of Steatohepatitis in Mice

추가적으로, 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 시간.

그후, 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. 후에 48 weeks of Retatrutide treatment, liver fat decreased by 51.3% (1 mg), 59% (4 mg), 그리고 86% (12 mg), 비교하다 4.6% in the control group.

궁극적으로, all treated patients achieved normal liver fat levels.

COA

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MS

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