Retatrutide
  • Retatrutide
  • Retatrutide

Retatrutide | CAS 2381089-83-2

  • cas：2381089-83-2
  • Molecular Formula：
  • Purity：99%
  • Molecular Weight：
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This product is for research and development use only.

Product Details;

CasNo： 2381089-83-2

Reliable factory customized supply Retatrutide 2381089-83-2

  • Molecular Formula:
  • Molecular Weight:

Retatrutide Chemical Properties

storage temp. 

 -20°C

solubility 

 Acetonitrile: Slightly soluble
DMSO: Sparingly Soluble: 1-10mg/mLPBS (pH 7.2): Sparingly Soluble: 1-10mg/mL
Water: Slightly soluble

form 

 powder

color 

 White lyophilized

Water Solubility 

 Soluble in water (5mg/ml).

Retatrutide Usage And Synthesis

Description

 Retatrutide is a novel triple agonist peptide of the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR) and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide inhibits human GCGR, GIPR and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively and mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively. It is an important tool for obesity research.
Retatrutide potently activates the GLP-1R signaling pathway to stimulate glucose-dependent insulin secretion through activity at the GIP receptor (GIPR) or the GLP-1R.
Retatrutide is a synthetic peptide with glucose-lowering effects. It is an antidiabetic agent against type 2 diabetes (T2D), stimulating insulin and suppressing glucagon secretion in a glucose-dependent manner.
Retatrutide was also shown to delay gastric emptying, lower fasting and postprandial glucose concentration, decrease food intake and reduce body weight in patients with type 2 diabetes.

History

 Retatrutide (LY-3437943) was discovered by the American pharmaceutical company Eli Lilly and Company. It is a triple glucagon hormone receptor agonist (GLP-1, GIP, and GCGR receptors) for obesity. The 2024 Lasker~DeBakey Clinical Medical Research Award has been given to Joel Habener and Svetlana Mojsov for their discovery of a new hormone GLP-1(7-37) and to Lotte Knudsen for her role in developing sustained acting versions of this hormone as a treatment for obesity.

Uses

 Retatrutide is a once-weekly triple hormone receptor agonist developed by Eli Lilly and Company. It is a single-molecule peptide consisting of 39 amino acids with a molecular weight of approximately 4,731.33 Da. Its amino acid sequence has been optimised to achieve balanced agonist activity at the glucose-dependent insulinotropic polypeptide receptor (GIPR), glucagon-like peptide-1 receptor (GLP-1R), and glucagon receptor (GCGR). By simultaneously targeting all three receptors, retatrutide provides a multifaceted approach to metabolic regulation. Activation of the GLP-1 pathway suppresses appetite and delays gastric emptying, GIP signalling enhances insulin sensitivity and supports lipid metabolism, while GCGR activation increases energy expenditure and promotes hepatic fat oxidation. The complementary actions of these pathways enable comprehensive regulation of energy intake, metabolic efficiency, and energy expenditure, contributing to substantial weight loss and metabolic improvement.

Biological Activity

 Retatrutide (LY3437943), a single peptide conjugated to a lipid diacid molecule, exerts a powerful agonist effect on the human glucagon‐receptor (GCGR), GIPR, and GLP‐1R. In comparison with the human glucagon and glucagon‐like peptide 1 (GLP‐1), retatrutide exhibits reduced potency (by a factor of 0.3 and 0.4, respectively) on the GCGR and GLP‐1R while displaying enhanced potency at the human GIPR (by a factor of 8.9) when compared to the glucose‐dependent insulinotropic polypeptide (GIP)[7].

in vitro

 In vitro, Retatrutide demonstrates similar efficacy to natural glucagon in evoking glucose production within hepatocytes. Meanwhile, in adipocytes, it surpasses native GIP in inducing lipolysis. Retatrutide is effective in reducing weight in individuals with nonsyndromic obesity. Retatrutide demonstrates dosage‐dependent pharmacokinetics, featuring a favourable half‐life of nearly 6 days, enabling convenient weekly administration. Additionally, GLP‐1 and GCG are known to significantly delay GE in humans, while GIP may have no impact on GE. Delayed GE reduces food consumption and, therefore, leads to weight reduction[7].

Clinical claims and research
Drug Target(s) Mechanism of Action Advantages Representative Clinical Outcomes
Semaglutide GLP-1 Receptor Mimics endogenous GLP-1 by delaying gastric emptying, enhancing satiety, stimulating glucose-dependent insulin secretion, and suppressing glucagon release. Once-weekly administration, potent appetite suppression, and proven cardiovascular protection. Reduces the risk of major adverse cardiovascular events (MACE) by approximately 26% and promotes significant weight loss.
Tirzepatide GIP + GLP-1 Receptors Simultaneously activates GIP and GLP-1 receptors, improving insulin secretion, glucose regulation, and energy metabolism. Superior glucose-lowering and weight-loss efficacy compared with GLP-1 receptor agonists alone. Demonstrated greater efficacy than semaglutide in head-to-head studies and reduced the apnoea–hypopnoea index (AHI) by up to 62.8% in patients with obstructive sleep apnoea.
Mazdutide GLP-1 + GCGR Receptors Combines appetite suppression through GLP-1 receptor activation with increased energy expenditure and lipid oxidation through glucagon receptor activation. Particularly beneficial for metabolic dysfunction-associated steatotic liver disease (MASLD) and hyperuricaemia. Reported fatty liver remission rates of approximately 41%, alongside substantial weight reduction.
Retatrutide GIP + GLP-1 + GCGR Receptors Simultaneously activates three metabolic pathways, combining appetite suppression with enhanced calorie expenditure. Currently among the most potent incretin-based therapies for weight management. Achieved mean weight loss of up to 28.7% at 68 weeks and significantly improved obesity-related complications, including knee osteoarthritis symptoms.

Semaglutide

 GLP-1 Receptor

Tirzepatide

 GIP + GLP-1 Receptors

Mazdutide

 GLP-1 + GCGR Receptors

Retatrutide

 GIP + GLP-1 + GCGR Receptors

References

 [1] LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept: T. Coskun, et al.; Cell Metab. 34, 1234 (2022) DOI:10.1016/j.cmet.2022.07.013
[2] The novel GIP, GLP-1 and glucagon receptor agonist retatrutide delays gastric emptying: S. Urva, et al.; Diabetes Obes. Metab. 25, 2784 (2023) DOI:10.1111/dom.15167
[3] LY3437943, a novel triple GIP, GLP-1, and glucagon receptor agonist in people with type 2 diabetes: a phase 1b, multicentre, double-blind, placebo-controlled, randomised, multiple-ascending dose trial: S. Urva, et al.; Lancet 400, 1869 (2022) DOI:10.1016/S0140-6736(22)02033-5
[4] Is retatrutide (LY3437943), a GLP-1, GIP, and glucagon receptor agonist a step forward in the treatment of diabetes and obesity S.A. Doggrell; Expert Opin. Investig. Drugs 32, 355 (2023) DOI:10.1080/13543784.2023.2206560
[5] Differentiation of human subcutaneous adipocytes and measurement of lipolytic function induced by GIP or LY3437943: A. Regmi & W. Roell; STAR Protoc. 4, 102304 (2023) DOI:10.1016/j.xpro.2023.102304
[6] Gut hormone co-agonists for the treatment of obesity: from bench to bedside: R. Nogueiras, et al.; Nature Metab. 5, 933 (2023) (Review) DOI:10.1038/s42255-023-00812-z
[7] Muhammad Naeem, Umm E Salma Shabbar Banatwala, Laiba Imran. “Unleashing the power of retatrutide: A possible triumph over obesity and overweight: A correspondence.” Health Science Reports 7 2 (2024).

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