1. GPCR/G Protein
  2. GLP Receptor GCGR
  3. Retatrutide TFA

Retatrutide TFA  (Synonyms: LY3437943 TFA)

Cat. No.: HY-P3506A Purity: 99.31%
COA Handling Instructions

Retatrutide (LY3437943) TFA is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide TFA binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide TFA can be used for the research of obesity.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Retatrutide TFA Chemical Structure

Retatrutide TFA Chemical Structure

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5 mg USD 750 In-stock
10 mg USD 1200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Retatrutide (LY3437943) TFA is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide TFA binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide TFA can be used for the research of obesity[1].

IC50 & Target

EC50 (for human): 5.79 (GCGR), 0.0643 (GIPR), 0.775 nM (GLP-1R)[1].
EC50 (for mouse): 2.32 (GCGR), 0.191 (GIPR), 0.794 nM (GLP-1R) [1].
Ki (for human): 5.6 (GCGR), 0.057 (GIPR), 7.2 nM (GLP-1)[1].

In Vitro

Retatrutide (LY3437943) TFA has efficacy for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively[1].
Retatrutide has efficacy for mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively[1].
Retatrutide has binding affinity for human GCGR, GIPR, and GLP-1R with Ki values of 5.6, 0.057 and 7.2 nM, respectively[1].
Retatrutide has binding affinity for mouse GCGR, GIPR, and GLP-1R with Ki values of 73, 2.8 and 1.3 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Retatrutide (LY3437943) TFA (s.c.; 0.47 mg/kg; single) engages GCGR in vivo and can improve glucose tolerance in an ipGTT through either the GIP or GLP-1 receptors[1].
Retatrutide (s.c.; 10 mL/kg; cycle every 3 days; for 21 days) causes great body weight loss and increases energy expenditure through glucagon receptor activatio[1].
Retatrutide has safety and tolerability[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

4731.33 (free base)

Formula

C221H342N46O68.xC2HF3O2

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL

H2O : 20 mg/mL (ultrasonic and adjust pH to 9 with NH3·H2O)

*"≥" means soluble, but saturation unknown.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (Infinity mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1.25 mg/mL (Infinity mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.31%

References
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Retatrutide TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Retatrutide TFA
Cat. No.:
HY-P3506A
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