2. GPCR/G Protein
  3. GCGR GLP Receptor
  4. Retatrutide

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

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CAS No. : 2381089-83-2

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Based on 3 publication(s) in Google Scholar

Other Forms of Retatrutide:

Retatrutide Related Antibodies

Top Publications Citing Use of Products
In Vivo Efficacy Study
Histological Imaging/Staining
IHC

    Retatrutide purchased from MedChemExpress. Usage Cited in: NPJ Metab Health Dis. 2025;3(1):10.  [Abstract]

    Mice were subcutaneously administered either Veh, 30 nmol/kg Retatrutide, or 30 nmol/kg SEMA every other day before the initiation of the dark cycle at 5 pm. Survival curves were plotted as % of mice tumor-free for each group.

    Retatrutide purchased from MedChemExpress. Usage Cited in: NPJ Metab Health Dis. 2025;3(1):10.  [Abstract]

    Mice were subcutaneously administered either Veh, 30 nmol/kg Retatrutide, or 30 nmol/kg SEMA every other day before the initiation of the dark cycle at 5 pm. Frequencies of CD45+ cells/live cells were shown.

    Retatrutide purchased from MedChemExpress. Usage Cited in: Endocrine. 2025 Jan;87(1):159-169.  [Abstract]

    The mice received daily subcutaneous injections of 10 nmol/kg of Retatrutide for 10 weeks. Changes in fasting blood glucose (FBG) of mice in each group were recorded.

    Retatrutide purchased from MedChemExpress. Usage Cited in: Endocrine. 2025 Jan;87(1):159-169.  [Abstract]

    The mice received daily subcutaneous injections of 10 nmol/kg of Retatrutide for 10 weeks. Representative HE and PAS stained images of the kidneys of mice in each group were obtained.

    Retatrutide purchased from MedChemExpress. Usage Cited in: Endocrine. 2025 Jan;87(1):159-169.  [Abstract]

    The mice received daily subcutaneous injections of 10 nmol/kg of Retatrutide for 10 weeks. Representative immunohistochemical staining of TNF-α, Caspase-1, NLRP3, fibronectin, collagen I, and α-SMA in renal tissue of mice in each group was performed.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide 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-1R) [1].
    Ki (for mouse): 73 (GCGR), 2.8 (GIPR), 1.3 nM (GLP-1R)[1].
    In Vitro

    Retatrutide (LY3437943) 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.

    Retatrutide Related Antibodies
    In Vivo

    Retatrutide (LY3437943) (s.c.; 47 μg/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.

    Animal Model: Male CD-1 mice[1]
    Dosage: 47 μg/kg
    Administration: Subcutaneous administration, single
    Result:
    AUClast, ng*h/mL AUC0-∞, ng*h/mL Cmax, ng/mL Tmax, h t1/2, h CLF, mL/h/kg
    41135 41905 1680 12 21 11.22
    Animal Model: Diet-induced obese (DIO) male C57/Bl6 mice (24-25 weeks, 40-51 g)[1]
    Dosage: 10 mL/kg
    Administration: Subcutaneous (SC) injection, cycle every 3 days, for 21 days
    Result: Decreased body weight and improved glycemic control.
    Molecular Weight

    4731.33

    Formula

    C221H342N46O68
    CAS No.
    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
    Sequence Shortening

    Y-{Aib}-QGTFTSDYSI-{α-Me-Leu}-LDK-{Lys(AEEA-γGlu-C20 diacid)}AQ-{Aib}-AFIEYLLEGGPSSGAPPPS-NH2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Sealed storage, away from moisture and light, under nitrogen

    Powder -80°C 2 years
    -20°C 1 year

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (10.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 20 mg/mL (4.23 mM; ultrasonic and adjust pH to 9 with NH3·H2O)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.2114 mL 1.0568 mL 2.1136 mL
    5 mM 0.0423 mL 0.2114 mL 0.4227 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    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: 99.96%

    SDS (252 KB)

    COA (273 KB) RP-HPLC (263 KB) MS (69 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 0.2114 mL 1.0568 mL 2.1136 mL 5.2839 mL
    DMSO 5 mM 0.0423 mL 0.2114 mL 0.4227 mL 1.0568 mL
    10 mM 0.0211 mL 0.1057 mL 0.2114 mL 0.5284 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Retatrutide 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.

    Keywords:

    Retatrutide2381089-83-2LY3437943LY 3437943LY-3437943GCGRGLP ReceptorGlucagon Receptorpeptideglucagon receptor (GCGR)glucosedependent insulinotropic polypeptide receptor (GIPR)glucagon-like peptide-1 receptor (GLP-1R)obesityInhibitorinhibitorinhibit

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