Retatrutide

Retatrutide is a revolutionary peptide targeting three key metabolic receptors.

 

გააზიარე შენი სიყვარული

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), და გლუკაგონის მსგავსი პეპტიდ-1 რეცეპტორი (GLP-1R). This new peptide drug shows strong potential in treating obesity-related metabolic disorders and type 2 diabetes due to its unique structure.

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

დამატებით, the attachment of a C20 fatty diacid chain a ლიზინი residue extends its ნახევარგამოყოფის პერიოდი and improves its pharmacological profile. Together, these advanced features support once-weekly subcutaneous dosing.

თანმიმდევრობა

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

CAS ნომერი

2381089-83-2

მოლეკულური ფორმულა

C221H342N46O68

მოლეკულური წონა

4731.33 გ/მოლ

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 for 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:

აღსანიშნავია, Retatrutide delayed GE in a glucose-dependent manner. In particular, 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. შედეგად, it supports effective obesity treatment.

4)Clinical Trial Weight Loss Results:

მაგალითად, a Phase 2 clinical trial reported significant weight loss in overweight and obese adults: 17.5% at 24 weeks and 24.4% at 48 კვირები.

2. Treats Type 2 შაქრიანი დიაბეტი

  • 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. In contrast, no other diabetes drug reached 50% efficacy.
  • These findings clearly demonstrate Retatrutide’s superior effectiveness in managing type 2 შაქრიანი დიაბეტი. თუმცა, the most common side effects were gastrointestinal.
  • ამავე დროს, in obese adults, Retatrutide treatment also led to significant weight loss over 48 კვირები.

3. Promotes Energy Expenditure

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

2)Reversal of Steatohepatitis in Mice:

დამატებით, 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 საათები.

Subsequently, 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. After 48 weeks of Retatrutide treatment, liver fat decreased by 51.3% (1 მგ), 59% (4 მგ), და 86% (12 მგ), compared to 4.6% in the control group.

Ultimately, all treated patients achieved normal liver fat levels.

COA

HPLC

MS

(1) Katsi, ვ.; Koutsopoulos, გ.; Fragoulis, C.; Dimitriadis, კ.; Tsioufis, კ. Retatrutide—A Game Changer in Obesity Pharmacotherapy. Biomolecules 2025, 15 (6). DOI: 10.3390/biom15060796.

(2) Naeem, ჰ.; Akram, ს.; Tarar, რ. ა.; Javed, მ. ა.; Shahid, მ. ბ.; Shehryar, მ.; Rehman, ზ. უ.; Siddiqui, მ. ა.; Ayub, ს.; Irfan, ა.; და სხვ. Retatrutide, a Trigonal Glp-1, Gip and Glucagon Receptor Agonist, and Its Role in Weight Reduction. კარდიოლოგიის ამერიკული კოლეჯის ჟურნალი 2024, 83 (13). DOI: 10.1016/s0735-1097(24)03892-0.

(3) ლი, ვ.; ჯოუ, ქ.; კონგ, ზ.; იუანი, ქ.; ლი, ვ.; ჟაო, ფ.; ქსუ, ჰ. ე.; ჟაო, ლ.-ჰ.; რომელიც, დ.; ვანგ, მ.-ვ. სტრუქტურული შეხედულებები სამმაგი აგონიზმზე GLP-1R-ში, GIPR და GCGR გამოიხატება რეტატრუტიდით. უჯრედის აღმოჩენა 2024, 10 (1). DOI: 10.1038/s41421-024-00700-0.

(4) Sanyal, ა. ჯ.; Kaplan, ლ. მ.; Frias, ჯ. პ.; Brouwers, ბ.; ვუ, ქ.; Thomas, მ. კ.; Harris, C.; Schloot, ნ. C.; Du, ი.; Mather, კ. ჯ.; და სხვ. Triple hormone receptor agonist retatrutide for metabolic dysfunction-associated steatotic liver disease: a randomized phase 2a trial. ბუნების მედიცინა 2024, 30 (7), 2037-2048. DOI: 10.1038/s41591-024-03018-2.

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