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

Retatrutide  (Synonyms: LY3437943)

Cat. No.: HY-P3506 Purity: 99.89%
COA Handling Instructions

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.

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

Custom Peptide Synthesis

Retatrutide Chemical Structure

Retatrutide Chemical Structure

CAS No. : 2381089-83-2

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1 mg USD 300 In-stock
5 mg USD 750 In-stock
10 mg USD 1200 In-stock
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Based on 1 publication(s) in Google Scholar

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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.

In Vivo

Retatrutide (LY3437943) (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.

Animal Model: Male CD-1 mice[1]
Dosage: 0.47 mg/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.
Clinical Trial
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

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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

Dosage

mg/kg

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(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: 99.89%

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.

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Retatrutide
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