Retatrutide LY3437943 - Buy Retatrutide

Retatrutide (LY3437943): Triple Receptor Agonist for Obesity and Metabolic Research

Product Overview
Retatrutide (LY3437943) is a potent, long-acting triple agonist peptide designed to target three critical metabolic receptors: the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). This advanced peptide binds with high affinity to human GCGR, GIPR, and GLP-1R, with EC₅₀ values of 5.79 nM, 0.0643 nM, and 0.775 nM, respectively. Retatrutide is currently under clinical investigation for its effectiveness in treating obesity, type 2 diabetes, and related metabolic disorders.
Mechanism of Action

Retatrutide acts by simultaneously activating three metabolic pathways that regulate glucose metabolism, energy balance, and appetite control:

GCGR Activation: Enhances energy expenditure and lipid metabolism.

GIPR Activation: Boosts insulin secretion in a glucose-dependent manner.

GLP-1R Activation: Promotes satiety, delays gastric emptying, and improves insulin sensitivity.

In Vitro Insights

Retatrutide exhibits strong receptor engagement across human and mouse models:

Human EC₅₀ Values: GCGR (5.79 nM), GIPR (0.0643 nM), GLP-1R (0.775 nM)

Mouse EC₅₀ Values: GCGR (2.32 nM), GIPR (0.191 nM), GLP-1R (0.794 nM)

High binding affinity (Ki values) further supports its receptor-targeting capabilities, particularly GIPR (0.057 nM in humans).

In Vivo Efficacy

Animal studies have demonstrated that Retatrutide:

Significantly improves glucose tolerance via GIP and GLP-1 pathways.

Induces substantial weight loss and increases energy expenditure in diet-induced obese (DIO) mouse models.

Offers a favorable pharmacokinetic profile with a half-life of ~21 hours post subcutaneous administration.

Clinical Development

Retatrutide is undergoing Phase 1 to Phase 3 clinical trials for several conditions, including:

Obesity and overweight

Type 2 diabetes mellitus

Chronic kidney disease

Obstructive sleep apnea

Knee osteoarthritis

Sponsor: Eli Lilly and Company
Notable Clinical Trials: NCT05931367, NCT05929066, NCT05882045
Product Details

Molecular Formula: C₂₂₁H₃₄₂N₄₆O₆₈

Molecular Weight: 4731.33 g/mol

CAS Number: 2381089-83-2

Appearance: White to off-white solid

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

Storage & Handling

Powder:

Store at -80°C (up to 2 years)

Store at -20°C (up to 1 year)

In Solution:

Stable at -80°C for 6 months

Stable at -20°C for 1 month

Protection: Store sealed, away from moisture, light, and under nitrogen atmosphere.

Shipping: Ships at room temperature within the continental US; international conditions may vary.

Note: This product is intended for research use only. Not for human or veterinary use.